Dr. Kenneth A Jacobson, PhD - National Institutes of Health - Chief, Molecular Recognition Section, Laboratory of Bioorganic Chemistry, NIDDK

Dr. Kenneth A Jacobson

PhD

National Institutes of Health

Chief, Molecular Recognition Section, Laboratory of Bioorganic Chemistry, NIDDK

Bethesda, MD | United States

Main Specialties: Chemistry

Additional Specialties: medicinal chemistry, pharmacology

Dr. Kenneth A Jacobson, PhD - National Institutes of Health - Chief, Molecular Recognition Section, Laboratory of Bioorganic Chemistry, NIDDK

Dr. Kenneth A Jacobson

PhD

Introduction

Kenneth A. Jacobson, Ph.D. is the John W. Daly Distinguished Investigator and Chief of the Molecular Recognition Section, Laboratory of Bioorganic Chemistry at the National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health in Bethesda, Maryland, USA. Dr. Jacobson is a medicinal chemist with interests in the structure and pharmacology of G protein-coupled receptors, in particular receptors for adenosine and for purine and pyrimidine nucleotides.

Primary Affiliation: National Institutes of Health - Bethesda, MD , United States

Specialties:

Additional Specialties:

Research Interests:

Education

University of California San Diego
PhD
Reed College
BA

Experience

National Institutes of Health
Senior Investigator
National Institute of Diabetes & DIgestive & Kidney Diseases

Publications

1017Publications

3145Reads

36Profile Views

2375PubMed Central Citations

Evidence for the Interaction of A Adenosine Receptor Agonists at the Drug-Binding Site(s) of Human P-glycoprotein (ABCB1).

Mol Pharmacol 2019 Aug 24;96(2):180-192. Epub 2019 May 24.

Laboratory of Cell Biology, Center for Cancer Research, National Cancer Institute (B.A., S.R.D., M.M., S.V., S.V.A.), and Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases (D.K.T., K.A.J.), National Institutes of Health, Bethesda, Maryland

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1124/mol.118.115295DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6608608PMC
August 2019
4 Reads
4.128 Impact Factor

Deficiency of adenosine deaminase 2 triggers adenosine-mediated NETosis and TNF production in patients with DADA2.

Blood 2019 Jul 23;134(4):395-406. Epub 2019 Apr 23.

Systemic Autoimmunity Branch, Intramural Research Program, National Institute of Arthritis and Musculoskeletal and Skin Diseases, National Institutes of Health, Bethesda, MD.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1182/blood.2018892752DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6659253PMC
July 2019
2 Reads
10.452 Impact Factor

Structure-Activity Relationship of Purine and Pyrimidine Nucleotides as Ecto-5'-Nucleotidase (CD73) Inhibitors.

J Med Chem 2019 Apr 21;62(7):3677-3695. Epub 2019 Mar 21.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases , National Institutes of Health , Bethesda , Maryland 20892 , United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.9b00164DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6526958PMC
April 2019
3 Reads
5.447 Impact Factor

Historical and Current Adenosine Receptor Agonists in Preclinical and Clinical Development.

Front Cell Neurosci 2019 28;13:124. Epub 2019 Mar 28.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.3389/fncel.2019.00124DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6447611PMC
March 2019
3 Reads
4.289 Impact Factor

Physiology and effects of nucleosides in mice lacking all four adenosine receptors.

PLoS Biol 2019 Mar 1;17(3):e3000161. Epub 2019 Mar 1.

Diabetes, Endocrinology, and Obesity Branch, National Institute of Diabetes and Digestive and Kidney Diseases, NIH, Bethesda, Maryland, United States of America.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1371/journal.pbio.3000161DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6415873PMC
March 2019
2 Reads

Structure Activity Relationship of 4-Amino-2-thiopyrimidine Derivatives as Platelet Aggregation Inhibitors.

Med Chem 2019 Feb 8. Epub 2019 Feb 8.

Unità di Medicina III, Azienda Ospedaliera San Paolo, Dipartimento di Medicina Chirurgia e Odontoiatria, Università di Milano, Via di Rudinì 8, I-20142 Milano. Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.2174/1573406415666190208124534DOI Listing
February 2019
2 Reads
1.387 Impact Factor

Editorial: Purinergic Pharmacology.

Front Pharmacol 2019 23;10:21. Epub 2019 Jan 23.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.3389/fphar.2019.00021DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6351471PMC
January 2019
13 Reads

Thermostabilization and purification of the human dopamine transporter (hDAT) in an inhibitor and allosteric ligand bound conformation.

PLoS One 2018 2;13(7):e0200085. Epub 2018 Jul 2.

Vollum Institute, Oregon Health & Science University, Portland, Oregon, United States of America.

View Article

Download full-text PDF

Source
http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0200085PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6028122PMC
January 2019
5 Reads
3.234 Impact Factor

Probing structure-activity relationship in β-arrestin2 recruitment of diversely substituted adenosine derivatives.

Biochem Pharmacol 2018 12 4;158:103-113. Epub 2018 Oct 4.

Laboratory of Toxicology, Department of Bioanalysis, Faculty of Pharmaceutical Sciences, Ghent University, Campus Heymans, Ottergemsesteenweg 460, B-9000 Ghent, Belgium. Electronic address:

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00062952183041
Publisher Site
http://dx.doi.org/10.1016/j.bcp.2018.10.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6530469PMC
December 2018
8 Reads
5.010 Impact Factor

Structure activity relationship of 2-arylalkynyl-adenine derivatives as human A adenosine receptor antagonists.

Medchemcomm 2018 Nov 18;9(11):1920-1932. Epub 2018 Oct 18.

Molecular Recognition Section , Laboratory of Bioorganic Chemistry , National Institute of Diabetes and Digestive and Kidney Diseases , National Institutes of Health , Bldg. 8A, Rm. B1A-19, NIH, NIDDK, LBC , Bethesda , Maryland 20892-0810 , USA . Email: ; ; Tel: +301 496 9024.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1039/c8md00317cDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6256369PMC
November 2018
2 Reads
2.495 Impact Factor

Preclinical Evaluation of the First Adenosine A Receptor Partial Agonist Radioligand for Positron Emission Tomography Imaging.

J Med Chem 2018 11 13;61(22):9966-9975. Epub 2018 Nov 13.

Laboratory of Neuroimaging , National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health , Bethesda , Maryland 20892-1013 , United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.8b01009DOI Listing
November 2018
15 Reads
5.450 Impact Factor

Repurposing of a Nucleoside Scaffold from Adenosine Receptor Agonists to Opioid Receptor Antagonists.

ACS Omega 2018 Oct 4;3(10):12658-12678. Epub 2018 Oct 4.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, 9000 Rockville Pike, Bethesda, Maryland 20892, United States.

View Article

Download full-text PDF

Source
http://pubs.acs.org/doi/10.1021/acsomega.8b01237
Publisher Site
http://dx.doi.org/10.1021/acsomega.8b01237DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6210068PMC
October 2018
3 Reads

Activation of adenosine A or A receptors causes hypothermia in mice.

Neuropharmacology 2018 09 13;139:268-278. Epub 2018 Mar 13.

Diabetes, Endocrinology, and Obesity Branch, National Institute of Diabetes and Digestive and Kidney Diseases, NIH, Bethesda, MD 20892, USA. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.neuropharm.2018.02.035DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6067974PMC
September 2018
41 Reads
1 Citation
5.110 Impact Factor

Remote control of movement disorders using a photoactive adenosine A receptor antagonist.

J Control Release 2018 08 31;283:135-142. Epub 2018 May 31.

Unitat de Farmacologia, Departament Patologia i Terapéutica Experimental, IDIBELL, Universitat de Barcelona, L'Hospitalet de Llobregat, Spain; Institut de Neurociències, Universitat de Barcelona, Spain. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.jconrel.2018.05.033DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6098950PMC
August 2018
3 Reads
7.705 Impact Factor

Author Correction: Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y and P2Y receptors.

Sci Rep 2018 Jul 24;8(1):11380. Epub 2018 Jul 24.

iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1038/s41598-018-29406-6DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6056558PMC
July 2018
1 Read
5.080 Impact Factor

Activation of basal forebrain purinergic P2 receptors promotes wakefulness in mice.

Sci Rep 2018 Jul 16;8(1):10730. Epub 2018 Jul 16.

Psychiatry, VA Boston Healthcare System and Harvard Medical School, West Roxbury, MA, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1038/s41598-018-29103-4DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6048041PMC
July 2018
17 Reads
5.080 Impact Factor

A binding kinetics study of human adenosine A receptor agonists.

Biochem Pharmacol 2018 07 3;153:248-259. Epub 2018 Jan 3.

Division of Medicinal Chemistry, LACDR, Leiden University, The Netherlands. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bcp.2017.12.026DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5959751PMC
July 2018
23 Reads
5.010 Impact Factor

Extrinsic Tryptophans as NMR Probes of Allosteric Coupling in Membrane Proteins: Application to the A Adenosine Receptor.

J Am Chem Soc 2018 07 20;140(26):8228-8235. Epub 2018 Jun 20.

Department of Integrative Structural and Computational Biology , The Scripps Research Institute , 10550 North Torrey Pines Road , La Jolla , California 92037 , United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jacs.8b03805DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6192543PMC
July 2018
1 Read
12.113 Impact Factor

A Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy.

Med Res Rev 2018 07 6;38(4):1031-1072. Epub 2017 Jul 6.

Department of Medical Sciences, Pharmacology Section, University of Ferrara, Via Fossato di Mortara 17/19, 44121, Ferrara, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1002/med.21456DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5756520PMC
July 2018
27 Reads
7 Citations
8.431 Impact Factor

Structure-Guided Modification of Heterocyclic Antagonists of the P2Y Receptor.

J Med Chem 2018 06 16;61(11):4860-4882. Epub 2018 May 16.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases , National Institutes of Health , Bethesda , Maryland 20892 , United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.8b00168DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6428052PMC
June 2018
4 Reads
1 Citation
5.450 Impact Factor

On the G protein-coupling selectivity of the native A adenosine receptor.

Biochem Pharmacol 2018 05 7;151:201-213. Epub 2017 Dec 7.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, 9000 Rockville Pike, Bethesda, MD 20892, USA. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bcp.2017.12.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5899946PMC
May 2018
9 Reads
2 Citations
5.010 Impact Factor

Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y and P2Y receptors.

Sci Rep 2018 May 24;8(1):8084. Epub 2018 May 24.

iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1038/s41598-018-26577-0DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5967328PMC
May 2018
4 Reads
5.080 Impact Factor

Species differences and mechanism of action of A adenosine receptor allosteric modulators.

Purinergic Signal 2018 03 23;14(1):59-71. Epub 2017 Nov 23.

Department of Pharmacology and Toxicology, Medical College of Wisconsin, 8701 Watertown Plank Road, Milwaukee, WI, 53226, USA.

View Article

Download full-text PDF

Source
http://link.springer.com/10.1007/s11302-017-9592-1
Publisher Site
http://dx.doi.org/10.1007/s11302-017-9592-1DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5842153PMC
March 2018
12 Reads
3.890 Impact Factor

Structural Connection between Activation Microswitch and Allosteric Sodium Site in GPCR Signaling.

Structure 2018 02 27;26(2):259-269.e5. Epub 2018 Jan 27.

Departments of Biological Sciences and Chemistry, Bridge Institute, USC Michelson Center, University of Southern California, 1002 West Childs Way, Los Angeles, CA 90089, USA. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.str.2017.12.013DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5810373PMC
February 2018
9 Reads
3 Citations
5.620 Impact Factor

Polypharmacology of conformationally locked methanocarba nucleosides.

Drug Discov Today 2017 12 3;22(12):1782-1791. Epub 2017 Aug 3.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes & Digestive & Kidney Diseases, National Institutes of Health, Bldg 8A, Rm B1A-19, Bethesda, MD 20892-0810, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.drudis.2017.07.013DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5705437PMC
December 2017
2 Reads
1 Citation
6.691 Impact Factor

Distinct Signaling Patterns of Allosteric Antagonism at the P2Y Receptor.

Mol Pharmacol 2017 11 1;92(5):613-626. Epub 2017 Sep 1.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1124/mol.117.109660DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5635520PMC
November 2017
4 Reads
2 Citations
4.130 Impact Factor

Highly selective A3 adenosine receptor agonists relieve chronic neuropathic pain.

Expert Opin Ther Pat 2017 08 20;27(8):967. Epub 2017 Jun 20.

b Laboratory of Bioorganic Chemistry, National Institute of Diabetes & Digestive & Kidney Diseases , National Institutes of Health , Bethesda , MD , USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1080/13543776.2017.1341018DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5605777PMC
August 2017
17 Reads
1 Citation
4.300 Impact Factor

Fragment optimization for GPCRs by molecular dynamics free energy calculations: Probing druggable subpockets of the A adenosine receptor binding site.

Sci Rep 2017 07 25;7(1):6398. Epub 2017 Jul 25.

Science for Life Laboratory, Department of Cell and Molecular Biology, Uppsala University, BMC, Box 596, SE-75124, Uppsala, Sweden.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1038/s41598-017-04905-0DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5526870PMC
July 2017
45 Reads
1 Citation
5.080 Impact Factor

Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.

J Med Chem 2017 04 20;60(7):3109-3123. Epub 2017 Mar 20.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Bethesda, Maryland 20892, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.7b00141DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5501184PMC
April 2017
29 Reads
4 Citations
5.450 Impact Factor

Hypothermia in mouse is caused by adenosine A and A receptor agonists and AMP via three distinct mechanisms.

Neuropharmacology 2017 03 30;114:101-113. Epub 2016 Nov 30.

Diabetes, Endocrinology, and Obesity Branch, National Institute of Diabetes and Digestive and Kidney Diseases, NIH, Bethesda, MD 20892, USA. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.neuropharm.2016.11.026DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5183552PMC
March 2017
56 Reads
11 Citations
5.110 Impact Factor

Structural Probing and Molecular Modeling of the A₃ Adenosine Receptor: A Focus on Agonist Binding.

Molecules 2017 Mar 11;22(3). Epub 2017 Mar 11.

Molecular Recognition Section (MRS), Laboratory of Bioorganic Chemistry, National Institutes of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MA 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.3390/molecules22030449DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5471610PMC
March 2017
2 Reads
5 Citations
2.420 Impact Factor

UDP-glucose promotes neutrophil recruitment in the lung.

Purinergic Signal 2016 12 15;12(4):627-635. Epub 2016 Jul 15.

Marsico Lung Institute/Cystic Fibrosis Research Center, University of North Carolina School of Medicine, 6007 Thurston-Bowles Building, CB 7248, Chapel Hill, NC, 27599-7248, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s11302-016-9524-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5124001PMC
December 2016
25 Reads
1 Citation
3.890 Impact Factor

Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT/5HT Serotonin Receptor Antagonists.

J Med Chem 2016 12 9;59(24):11006-11026. Epub 2016 Dec 9.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Bethesda, Maryland 20892, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.6b01183DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5201133PMC
December 2016
10 Reads
4 Citations
5.450 Impact Factor

Inherited dysfunctional platelet P2Y receptor mutations associated with bleeding disorders.

Hamostaseologie 2016 Nov 4;36(4):279-283. Epub 2016 Aug 4.

Katharina Machura, University Medical Center, Freiburg - Department of Pediatrics and Adolescent Medicine, Breisacher-Str. 66, 79106 Freiburg, Germany, Tel. +49/(0)761/27 06 37 10, E-mail:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.5482/HAMO-16-03-0010DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5099093PMC
November 2016
29 Reads
2 Citations
1.590 Impact Factor

Ocular Purine Receptors as Drug Targets in the Eye.

J Ocul Pharmacol Ther 2016 10 30;32(8):534-547. Epub 2016 Aug 30.

2 Departments of Physiology and Medicine, University of Pennsylvania Perelman School of Medicine , Philadelphia, Pennsylvania.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1089/jop.2016.0090DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5069731PMC
October 2016
8 Reads
3 Citations
1.420 Impact Factor

Structure-Based Screening of Uncharted Chemical Space for Atypical Adenosine Receptor Agonists.

ACS Chem Biol 2016 10 22;11(10):2763-2772. Epub 2016 Aug 22.

Science for Life Laboratory, Department of Medicinal Chemistry, BMC, Uppsala University , P.O. Box 574, SE-751 23 Uppsala, Sweden.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acschembio.6b00357DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5207038PMC
October 2016
4 Reads
5 Citations
5.331 Impact Factor

South (S)- and North (N)-Methanocarba-7-Deazaadenosine Analogues as Inhibitors of Human Adenosine Kinase.

J Med Chem 2016 07 13;59(14):6860-77. Epub 2016 Jul 13.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Bldg. 8A, Rm. B1A-19, Bethesda, Maryland 20892-0810, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.6b00689DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5032833PMC
July 2016
36 Reads
6 Citations
5.450 Impact Factor

Structure-Activity Analysis of Biased Agonism at the Human Adenosine A3 Receptor.

Mol Pharmacol 2016 07 2;90(1):12-22. Epub 2016 May 2.

Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria, Australia (J.-A.B., A.T.N.N., K.J.G., A.C., L.T.M); and Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Disease, National Institutes of Health, Bethesda, Maryland (S.P., D.K.T., K.A.J)

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1124/mol.116.103283DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4931866PMC
July 2016
35 Reads
8 Citations
4.130 Impact Factor

Structure-Based Design of 3-(4-Aryl-1H-1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y14 Receptor Antagonists.

J Med Chem 2016 07 22;59(13):6149-68. Epub 2016 Jun 22.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Bethesda, Maryland 20892-0810, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.6b00044DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4947982PMC
July 2016
13 Reads
1 Citation
5.450 Impact Factor

On the selectivity of the Gαq inhibitor UBO-QIC: A comparison with the Gαi inhibitor pertussis toxin.

Biochem Pharmacol 2016 May 5;107:59-66. Epub 2016 Mar 5.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, 9000 Rockville Pike, Bethesda, MD 20892, USA. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bcp.2016.03.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4839537PMC
May 2016
6 Citations
5.010 Impact Factor

Medicinal chemistry of adenosine, P2Y and P2X receptors.

Neuropharmacology 2016 05 12;104:31-49. Epub 2015 Dec 12.

PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, Bonn, Germany.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.neuropharm.2015.12.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4871727PMC
May 2016
32 Reads
24 Citations
5.110 Impact Factor

Rigid Adenine Nucleoside Derivatives as Novel Modulators of the Human Sodium Symporters for Dopamine and Norepinephrine.

J Pharmacol Exp Ther 2016 Apr 26;357(1):24-35. Epub 2016 Jan 26.

VA Portland Health Care System, Research Service (R&D-22), and Departments of Psychiatry and Behavioral Neuroscience, Oregon Health and Science University, Portland, Oregon (A.J., A.J.E.); and Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (D.K.T., K.A.J.).

View Article

Download full-text PDF

Source
http://jpet.aspetjournals.org/content/357/1/24.full.pdf
Web Search
http://jpet.aspetjournals.org/cgi/doi/10.1124/jpet.115.22966
Publisher Site
http://dx.doi.org/10.1124/jpet.115.229666DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4809312PMC
April 2016
12 Reads
5 Citations
3.972 Impact Factor

Identification of A3 adenosine receptor agonists as novel non-narcotic analgesics.

Br J Pharmacol 2016 Apr 6;173(8):1253-67. Epub 2016 Mar 6.

Department of Pharmacology and Physiology, Saint Louis University School of Medicine, St. Louis, MO, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1111/bph.13446DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4940822PMC
April 2016
1 Read
13 Citations
4.842 Impact Factor

Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists.

J Med Chem 2016 Apr 18;59(7):3249-63. Epub 2016 Feb 18.

Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Building 8A, Room B1A-19, Bethesda, Maryland 20892-0810, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.5b01998DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4970510PMC
April 2016
34 Reads
4 Citations
5.450 Impact Factor

Renal intercalated cells sense and mediate inflammation via the P2Y14 receptor.

PLoS One 2015 23;10(3):e0121419. Epub 2015 Mar 23.

Center for Systems Biology, Massachusetts General Hospital/Harvard Medical School, Boston, Massachusetts, United States of America; Program in Membrane Biology/Nephrology Division, Massachusetts General Hospital/Harvard Medical School, Boston, Massachusetts, United States of America.

View Article

Download full-text PDF

Source
http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0121419PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4370445PMC
February 2016
6 Reads
9 Citations
3.234 Impact Factor

Peripheral Adenosine A3 Receptor Activation Causes Regulated Hypothermia in Mice That Is Dependent on Central Histamine H1 Receptors.

J Pharmacol Exp Ther 2016 Feb 25;356(2):474-82. Epub 2015 Nov 25.

Diabetes, Endocrinology, and Obesity Branch (J.L.C., C.X., R.A.P., M.L.R.), Molecular Recognition Section, Laboratory of Bioorganic Chemistry (D.K.T., K.A.J.), and Mouse Metabolism Core (O.G.), National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland; and Department of Pharmacological and Physiological Science, Saint Louis University School of Medicine, St. Louis, Missouri (Z.C., D.S.)

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1124/jpet.115.229872DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4746492PMC
February 2016
43 Reads
11 Citations
3.972 Impact Factor

New paradigms in GPCR drug discovery.

Biochem Pharmacol 2015 Dec 8;98(4):541-55. Epub 2015 Aug 8.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bldg. 8A, Rm. B1A-19, Bethesda, Maryland 20892, USA. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bcp.2015.08.085DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4967540PMC
December 2015
31 Reads
20 Citations
5.010 Impact Factor

Design, synthesis, pharmacological characterization of a fluorescent agonist of the P2Y₁₄ receptor.

Bioorg Med Chem Lett 2015 Nov 10;25(21):4733-4739. Epub 2015 Aug 10.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2015.08.021DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4607650PMC
November 2015
9 Reads
3 Citations
2.420 Impact Factor

Lighting up G protein-coupled purinergic receptors with engineered fluorescent ligands.

Neuropharmacology 2015 Nov 16;98:58-67. Epub 2015 Apr 16.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, 20892 Bethesda, USA. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.neuropharm.2015.04.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4608850PMC
November 2015
5 Reads
2 Citations
5.110 Impact Factor

Efficient, large-scale synthesis and preclinical studies of MRS5698, a highly selective A3 adenosine receptor agonist that protects against chronic neuropathic pain.

Purinergic Signal 2015 Sep 27;11(3):371-87. Epub 2015 Jun 27.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD, 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s11302-015-9459-2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4529848PMC
September 2015
9 Reads
11 Citations
3.890 Impact Factor

Enhancement of glucose uptake in mouse skeletal muscle cells and adipocytes by P2Y6 receptor agonists.

PLoS One 2014 30;9(12):e116203. Epub 2014 Dec 30.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland, United States of America.

View Article

Download full-text PDF

Source
http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0116203PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4280206PMC
September 2015
7 Reads
4 Citations
3.234 Impact Factor

Metabolic mapping of A3 adenosine receptor agonist MRS5980.

Biochem Pharmacol 2015 Sep 23;97(2):215-23. Epub 2015 Jul 23.

Laboratory of Metabolism, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bcp.2015.07.007DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4581425PMC
September 2015
28 Reads
2 Citations
5.010 Impact Factor

Nucleotides Acting at P2Y Receptors: Connecting Structure and Function.

Mol Pharmacol 2015 Aug 2;88(2):220-30. Epub 2015 Apr 2.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institutes of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (K.A.J., S.P., Z.-G.G., E.K.); The Bridge Institute, Dana and David Dornsife School of Letters, Arts, and Sciences, University of Southern California, Los Angeles, California (V.K., R.C.S.); and Chinese Academy of Sciences Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China (B.W., Q.Z.).

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1124/mol.114.095711DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4518082PMC
August 2015
5 Reads
17 Citations
4.130 Impact Factor

Modeling ligand recognition at the P2Y12 receptor in light of X-ray structural information.

J Comput Aided Mol Des 2015 Aug 21;29(8):737-56. Epub 2015 Jul 21.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bldg. 8A, Rm. B1A-19, LBC, NIH, NIDDK, Bethesda, MD, 20892-0810, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s10822-015-9858-zDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4536181PMC
August 2015
41 Reads
3 Citations
2.990 Impact Factor

Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy.

ACS Med Chem Lett 2015 Jul 20;6(7):804-8. Epub 2015 May 20.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Bethesda, Maryland 20892-0810, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acsmedchemlett.5b00150DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4499829PMC
July 2015
14 Reads
7 Citations
3.120 Impact Factor

Molecular modeling of the human P2Y14 receptor: A template for structure-based design of selective agonist ligands.

Bioorg Med Chem 2015 Jul 21;23(14):4056-64. Epub 2015 Mar 21.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bldg. 8A, Rm. B1A-19, Bethesda, MD 20892-0810, USA. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmc.2015.03.042DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4468048PMC
July 2015
3 Reads
7 Citations
2.793 Impact Factor

A₃ adenosine receptor allosteric modulator induces an anti-inflammatory effect: in vivo studies and molecular mechanism of action.

Mediators Inflamm 2014 13;2014:708746. Epub 2014 Oct 13.

Can-Fite BioPharma Ltd., Kiryat-Matalon, 10 Bareket Street, P.O. Box 7537, 49170 Petach Tikva, Israel.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1155/2014/708746DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4211160PMC
July 2015
14 Reads
6 Citations
3.240 Impact Factor

John Daly Lecture: Structure-guided Drug Design for Adenosine and P2Y Receptors.

Comput Struct Biotechnol J 2015 16;13:286-98. Epub 2014 Oct 16.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892 USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.csbj.2014.10.004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4423517PMC
May 2015
35 Reads
4 Citations

Two disparate ligand-binding sites in the human P2Y1 receptor.

Nature 2015 Apr 30;520(7547):317-21. Epub 2015 Mar 30.

CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Pudong, Shanghai 201203, China.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1038/nature14287DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4408927PMC
April 2015
40 Reads
53 Citations
42.351 Impact Factor

P2X4 receptor-eNOS signaling pathway in cardiac myocytes as a novel protective mechanism in heart failure.

Comput Struct Biotechnol J 2015 7;13:1-7. Epub 2014 Nov 7.

Pat and Jim Calhoun Cardiology Center, University of Connecticut Medical Center, Farmington, CT, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.csbj.2014.11.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4348440PMC
March 2015
26 Reads

Molecular docking screening using agonist-bound GPCR structures: probing the A2A adenosine receptor.

J Chem Inf Model 2015 Mar 13;55(3):550-63. Epub 2015 Feb 13.

†Science for Life Laboratory, Stockholm University, Box 1031, SE-171 21 Solna, Sweden.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/ci500639gDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4474233PMC
March 2015
85 Reads
12 Citations
3.740 Impact Factor

A3 adenosine receptor agonist prevents the development of paclitaxel-induced neuropathic pain by modulating spinal glial-restricted redox-dependent signaling pathways.

Pain 2014 Dec 19;155(12):2560-7. Epub 2014 Sep 19.

Department of Pharmacological and Physiological Science, Saint Louis University School of Medicine, 1402 South Grand Blvd, St Louis, MO 63104, USA. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.pain.2014.09.016DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4529068PMC
December 2014
44 Reads
20 Citations
5.213 Impact Factor

Exploring a 2-naphthoic acid template for the structure-based design of P2Y14 receptor antagonist molecular probes.

ACS Chem Biol 2014 Dec 20;9(12):2833-42. Epub 2014 Oct 20.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Bethesda, Maryland 20892, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/cb500614pDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4273980PMC
December 2014
18 Reads
10 Citations
5.331 Impact Factor

In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.

J Med Chem 2014 Dec 25;57(23):9901-14. Epub 2014 Nov 25.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Building 8A, Room B1A-19, Bethesda, Maryland 20892-0810, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm501021nDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4266358PMC
December 2014
35 Reads
19 Citations
5.450 Impact Factor

Uncovering caffeine's adenosine A2A receptor inverse agonism in experimental parkinsonism.

ACS Chem Biol 2014 Nov 2;9(11):2496-501. Epub 2014 Oct 2.

Unitat de Farmacologia, Departament Patologia i Terapèutica Experimental, Facultat de Medicina, IDIBELL-Universitat de Barcelona , L'Hospitalet de Llobregat, 08907 Barcelona, Spain.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/cb5005383DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4245165PMC
November 2014
13 Reads
10 Citations
5.331 Impact Factor

Photomodulation of G protein-coupled adenosine receptors by a novel light-switchable ligand.

Bioconjug Chem 2014 Oct 2;25(10):1847-54. Epub 2014 Oct 2.

Institute for Bioengineering of Catalonia (IBEC) , 08028 Barcelona, Spain.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/bc5003373DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4198106PMC
October 2014
29 Reads
4 Citations
4.513 Impact Factor

Programmable nanoscaffolds that control ligand display to a G-protein-coupled receptor in membranes to allow dissection of multivalent effects.

J Am Chem Soc 2014 Sep 25;136(35):12296-303. Epub 2014 Aug 25.

Laboratory of Bioorganic Chemistry, NIDDK, ‡Laboratory of Biochemistry and Genetics, NIDDK, and §Laboratory of Cell Biology, CCR, NCI, National Institutes of Health , Bethesda, Maryland 20892, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/ja504288sDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4156868PMC
September 2014
32 Reads
5 Citations
12.113 Impact Factor

Portraying G protein-coupled receptors with fluorescent ligands.

ACS Chem Biol 2014 Sep 28;9(9):1918-28. Epub 2014 Jul 28.

Unitat de Farmacologia, Departament Patologia i Terapèutica Experimental, Facultat de Medicina, IDIBELL, Universitat de Barcelona , L'Hospitalet de Llobregat, 08907 Barcelona, Spain.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/cb5004042DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4168789PMC
September 2014
9 Reads
4 Citations
5.331 Impact Factor

The role of activated adenosine receptors in degranulation of human LAD2 mast cells.

Purinergic Signal 2014 Sep 5;10(3):465-75. Epub 2014 Mar 5.

Department of Physiology, University of Pennsylvania School of Medicine, A303 Richards Building, Philadelphia, PA, 19104-6085, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s11302-014-9409-4DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4152452PMC
September 2014
25 Reads
4 Citations
3.890 Impact Factor

Probing biased/partial agonism at the G protein-coupled A(2B) adenosine receptor.

Biochem Pharmacol 2014 Aug 20;90(3):297-306. Epub 2014 May 20.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, Blg. 8A, Rm B1 A-17, NDDK 8 Center Dr., 9000 Rockville Pike, Bethesda, MD 20892-0810, USA. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bcp.2014.05.008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4128710PMC
August 2014
5 Reads
8 Citations
5.010 Impact Factor

Rapid synthesis of alkoxyamine hydrochloride derivatives from alkyl bromide and di--butoxycarbonylhydroxylamine ((Boc)NOH).

Synth Commun 2014 Aug;44(16):2344-2347

National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1080/00397911.2014.895014DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4215731PMC
August 2014
22 Reads
1 Citation
0.930 Impact Factor

Extended N(6) substitution of rigid C2-arylethynyl nucleosides for exploring the role of extracellular loops in ligand recognition at the A3 adenosine receptor.

Bioorg Med Chem Lett 2014 Aug 11;24(15):3302-6. Epub 2014 Jun 11.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, USA. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2014.06.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4158450PMC
August 2014
9 Reads
3 Citations
2.420 Impact Factor

Synthesis and evaluation of N⁶-substituted apioadenosines as potential adenosine A₃ receptor modulators.

Bioorg Med Chem 2014 Aug 23;22(15):4257-68. Epub 2014 May 23.

Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Harelbekestraat 72, B-9000 Gent, Belgium. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmc.2014.05.036DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4128473PMC
August 2014
4 Reads
2 Citations
2.793 Impact Factor

Potential for developing purinergic drugs for gastrointestinal diseases.

Inflamm Bowel Dis 2014 Jul;20(7):1259-87

*Department of Anesthesiology, The Ohio State University Wexner Medical Center, Columbus, Ohio; and †Laboratory of Bioorganic Chemistry & Molecular Recognition Section, National Institute of Diabetes & Digestive & Kidney Diseases, National Institutes of Health, Bethesda, MD.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1097/MIB.0000000000000047DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4340257PMC
July 2014
27 Reads
22 Citations
4.464 Impact Factor

4-Alkyloxyimino derivatives of uridine-5'-triphosphate: distal modification of potent agonists as a strategy for molecular probes of P2Y2, P2Y4, and P2Y6 receptors.

J Med Chem 2014 May 18;57(9):3874-83. Epub 2014 Apr 18.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Bethesda, Maryland 20892 United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm500367eDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4018175PMC
May 2014
13 Reads
9 Citations
5.450 Impact Factor

Novel protective role of endogenous cardiac myocyte P2X4 receptors in heart failure.

Circ Heart Fail 2014 May 12;7(3):510-8. Epub 2014 Mar 12.

From Pat and Jim Calhoun Cardiology Center, University of Connecticut Medical Center, Farmington, CT (T.Y., J.S., R.Y., J.R., K.D.-K., J.G., B.T.L.); and Laboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, Bethesda, MD (K.A.J.).

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1161/CIRCHEARTFAILURE.113.001023DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4289151PMC
May 2014
27 Reads
8 Citations
5.891 Impact Factor

History of Chemistry in the National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK).

Bull Hist Chem 2014 Jan;39(2):150-165

Laboratory of Bioorganic Chemistry, National Institutes of Diabetes and Digestive and Kidney Diseases, NIH, Bethesda, MD 20892.

View Article

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4581437PMC
January 2014
2 Reads
1 Citation

Methanocarba ring as a ribose modification in ligands of G protein-coupled purine and pyrimidine receptors: synthetic approaches.

Medchemcomm 2013 Dec;2013(4):619-630

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1039/C2MD20348KDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4493925PMC
December 2013
3 Reads
4 Citations
2.500 Impact Factor

P2Y2 receptor agonist with enhanced stability protects the heart from ischemic damage in vitro and in vivo.

Purinergic Signal 2013 Dec 5;9(4):633-42. Epub 2013 Jul 5.

Cardiac Research Laboratory of the Department of Cardiothoracic Surgery, Felsenstein Medical Research Center, Rabin Medical Center, Tel Aviv University, Petach Tikva, Israel.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s11302-013-9374-3DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3889391PMC
December 2013
9 Reads
6 Citations
3.890 Impact Factor

Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain.

J Med Chem 2013 Jul 3;56(14):5949-63. Epub 2013 Jul 3.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Bethesda, Maryland 20892-0810, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm4007966DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3858399PMC
July 2013
7 Reads
18 Citations
5.450 Impact Factor

A selective high-affinity antagonist of the P2Y14 receptor inhibits UDP-glucose-stimulated chemotaxis of human neutrophils.

Mol Pharmacol 2013 Jul 16;84(1):41-9. Epub 2013 Apr 16.

Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, NC 27599, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1124/mol.113.085654DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3684828PMC
July 2013
5 Reads
21 Citations
4.130 Impact Factor

Dopamine D(2) receptor-mediated modulation of adenosine A(2A) receptor agonist binding within the A(2A)R/D(2)R oligomer framework.

Neurochem Int 2013 Jul 23;63(1):42-6. Epub 2013 Apr 23.

Unitat de Farmacologia, Departament de Patologia i Terapèutica Experimental, Facultat de Medicina, IDIBELL, Universitat de Barcelona, L'Hospitalet de Llobregat, 08907 Barcelona, Spain.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.neuint.2013.04.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3705641PMC
July 2013
27 Reads
5 Citations
3.092 Impact Factor

Probing GPCR structure: adenosine and P2Y nucleotide receptors.

Methods Enzymol 2013 ;520:199-217

Laboratory of Biological Modeling, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/B978-0-12-391861-1.00009-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3579568PMC
June 2013
17 Reads
1 Citation
2.090 Impact Factor

A2B adenosine receptor blockade inhibits growth of prostate cancer cells.

Purinergic Signal 2013 Jun 15;9(2):271-80. Epub 2013 Jan 15.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s11302-012-9350-3DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3646116PMC
June 2013
6 Reads
16 Citations
3.890 Impact Factor

Modulation of G protein-coupled adenosine receptors by strategically functionalized agonists and antagonists immobilized on gold nanoparticles.

Purinergic Signal 2013 Jun 20;9(2):183-98. Epub 2012 Nov 20.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, USA.

View Article

Download full-text PDF

Source
http://link.springer.com/content/pdf/10.1007/s11302-012-9338
Web Search
http://link.springer.com/10.1007/s11302-012-9338-z
Publisher Site
http://dx.doi.org/10.1007/s11302-012-9338-zDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3646115PMC
June 2013
34 Reads
4 Citations
3.890 Impact Factor

Limits of ligand selectivity from docking to models: in silico screening for A(1) adenosine receptor antagonists.

PLoS One 2012 21;7(11):e49910. Epub 2012 Nov 21.

Department of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, California, United States of America.

View Article

Download full-text PDF

Source
http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0049910PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3503826PMC
May 2013
27 Reads
13 Citations
3.230 Impact Factor

4-Alkyloxyimino-cytosine nucleotides: tethering approaches to molecular probes for the P2Y receptor.

Medchemcomm 2013 May;4:1156-1165

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, USA. ; Tel: +1 301-496-9024.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1039/C3MD00132FDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4493932PMC
May 2013
17 Reads
7 Citations
2.500 Impact Factor

Structure-based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates.

J Med Chem 2013 May 9;56(10):3749-67. Epub 2013 May 9.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Bethesda, Maryland 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm400422sDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3701956PMC
May 2013
3 Reads
11 Citations
5.450 Impact Factor

Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor.

Biochem Pharmacol 2013 Apr 31;85(8):1171-81. Epub 2013 Jan 31.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bcp.2013.01.021DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3604185PMC
April 2013
13 Reads
9 Citations
5.010 Impact Factor

AMP-activated protein kinase as regulator of P2Y(6) receptor-induced insulin secretion in mouse pancreatic β-cells.

Biochem Pharmacol 2013 Apr 17;85(7):991-8. Epub 2013 Jan 17.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bcp.2012.11.029DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3594329PMC
April 2013
3 Reads
7 Citations
5.010 Impact Factor

The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells.

Purinergic Signal 2013 Mar 24;9(1):31-40. Epub 2012 Jul 24.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, 9000 Rockville Pike, Bethesda, MD 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s11302-012-9325-4DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3568423PMC
March 2013
5 Reads
14 Citations
3.890 Impact Factor

5'-Phosphate and 5'-phosphonate ester derivatives of (N)-methanocarba adenosine with in vivo cardioprotective activity.

J Med Chem 2013 Feb 22;56(3):902-14. Epub 2013 Jan 22.

Molecular Recognition Section, National Institutes of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Bethesda, Maryland 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm301372cDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3574217PMC
February 2013
24 Reads
2 Citations
5.450 Impact Factor

Molecular determinants of A2AR-D2R allosterism: role of the intracellular loop 3 of the D2R.

J Neurochem 2012 Nov 28;123(3):373-84. Epub 2012 Sep 28.

Unitat de Farmacologia, Facultat de Medicina, Departament de Patologia i Terapèutica Experimental, Universitat de Barcelona, L'Hospitalet de Llobregat, Barcelona, Spain.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1111/j.1471-4159.2012.07956.xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3480334PMC
November 2012
9 Reads
17 Citations
4.280 Impact Factor

Structure-activity relationships and molecular modeling of 1,2,4-triazoles as adenosine receptor antagonists.

ACS Med Chem Lett 2012 Sep 30;3(9):715-720. Epub 2012 Jul 30.

Center for Biomembrane Research, Department of Biochemistry and Biophysics, Stockholm University, SE-10691 Stockholm, Sweden.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/ml300097gDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3549271PMC
September 2012
3 Reads
4 Citations
3.120 Impact Factor

Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity.

J Med Chem 2012 Sep 10;55(18):8075-90. Epub 2012 Sep 10.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm300965aDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3463139PMC
September 2012
13 Reads
18 Citations
5.450 Impact Factor

New insights for drug design from the X-ray crystallographic structures of G-protein-coupled receptors.

Mol Pharmacol 2012 Sep 13;82(3):361-71. Epub 2012 Jun 13.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institutes of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892-0810, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1124/mol.112.079335DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3422707PMC
September 2012
20 Reads
22 Citations
4.130 Impact Factor

G protein-coupled adenosine (P1) and P2Y receptors: ligand design and receptor interactions.

Purinergic Signal 2012 Sep 29;8(3):419-36. Epub 2012 Feb 29.

Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s11302-012-9294-7DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3360101PMC
September 2012
22 Reads
29 Citations
3.890 Impact Factor

Virtual screening leads to the discovery of novel non-nucleotide P2Y₁ receptor antagonists.

Bioorg Med Chem 2012 Sep 3;20(17):5254-61. Epub 2012 Jul 3.

Laboratory of Biological Modeling, National Institutes of Health, Bethesda, MD 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmc.2012.06.044DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3420346PMC
September 2012
3 Reads
4 Citations
2.790 Impact Factor

Farnesyl pyrophosphate is an endogenous antagonist to ADP-stimulated P2Y₁₂ receptor-mediated platelet aggregation.

Thromb Haemost 2012 Jul 25;108(1):119-32. Epub 2012 May 25.

Department of Cardiology, Lund University, Lund, Sweden.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1160/TH11-10-0749DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3479660PMC
July 2012
3 Reads
1 Citation
4.980 Impact Factor

Truncated Nucleosides as A(3) Adenosine Receptor Ligands: Combined 2-Arylethynyl and Bicyclohexane Substitutions.

ACS Med Chem Lett 2012 Jul 11;3(7):596-601. Epub 2012 Jun 11.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892-0810.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/ml300107eDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3491360PMC
July 2012
2 Reads
11 Citations
3.120 Impact Factor

Novel fluorescent antagonist as a molecular probe in A(3) adenosine receptor binding assays using flow cytometry.

Biochem Pharmacol 2012 Jun 1;83(11):1552-61. Epub 2012 Mar 1.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bcp.2012.02.019DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3322254PMC
June 2012
7 Reads
11 Citations
5.010 Impact Factor

Controlling murine and rat chronic pain through A3 adenosine receptor activation.

FASEB J 2012 May 17;26(5):1855-65. Epub 2012 Feb 17.

Department of Pharmacological and Physiological Science, St. Louis University School of Medicine, 1402 South Grand Blvd, St. Louis, MO 63104, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1096/fj.11-201541DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3336784PMC
May 2012
24 Reads
31 Citations
5.040 Impact Factor

Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions.

J Med Chem 2012 May 16;55(10):4847-60. Epub 2012 May 16.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health , Bethesda, Maryland 20892, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm300396nDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3371665PMC
May 2012
15 Reads
43 Citations
5.450 Impact Factor

Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.

J Med Chem 2012 May 30;55(9):4297-308. Epub 2012 Apr 30.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm300095sDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3479662PMC
May 2012
29 Reads
18 Citations
5.450 Impact Factor

Pharmacological and therapeutic effects of A3 adenosine receptor agonists.

Drug Discov Today 2012 Apr 19;17(7-8):359-66. Epub 2011 Oct 19.

Can-Fite BioPharma Ltd, Kiryat-Matalon, 10 Bareket St, PO Box 7537, Petah-Tikva 49170, Israel.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.drudis.2011.10.007DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3289754PMC
April 2012
4 Reads
58 Citations
6.690 Impact Factor

Synthesis and P2Y₂ receptor agonist activities of uridine 5'-phosphonate analogues.

Bioorg Med Chem 2012 Apr 15;20(7):2304-15. Epub 2012 Feb 15.

Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Ghent University, Harelbekestraat 72, B-9000 Gent, Belgium.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmc.2012.02.012DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3303979PMC
April 2012
3 Reads
3 Citations
2.790 Impact Factor

Click modification in the N6 region of A3 adenosine receptor-selective carbocyclic nucleosides for dendrimeric tethering that preserves pharmacophore recognition.

Bioconjug Chem 2012 Feb 11;23(2):232-47. Epub 2012 Jan 11.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/bc200526cDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3291892PMC
February 2012
13 Reads
3 Citations
4.510 Impact Factor

Emerging adenosine receptor agonists: an update.

Expert Opin Emerg Drugs 2011 Dec 7;16(4):597-602. Epub 2011 Dec 7.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1517/14728214.2011.644786DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3261781PMC
December 2011
1 Read
8 Citations
3.060 Impact Factor

Polyamidoamine (PAMAM) dendrimer conjugate specifically activates the A3 adenosine receptor to improve post-ischemic/reperfusion function in isolated mouse hearts.

BMC Pharmacol 2011 Oct 31;11:11. Epub 2011 Oct 31.

Department of Pharmacology/Toxicology and the Cardiovascular Center, Medical College of Wisconsin, 8701 Watertown Plank Road, Milwaukee, WI 53226, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1186/1471-2210-11-11DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3247180PMC
October 2011
9 Reads
4 Citations

Regio- and stereoselective synthesis of truncated 3'-aminocarbanucleosides and their binding affinity at the A3 adenosine receptor.

Org Biomol Chem 2011 Oct 23;9(20):6955-62. Epub 2011 Aug 23.

Laboratory of Medicinal Chemistry, College of Pharmacy and Department of Bioinspired Science, Ewha Womans University, Seoul, 120-750, Korea.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1039/c1ob05853cDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3616502PMC
October 2011
2 Reads
1 Citation

Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers.

Biochem Pharmacol 2011 Sep 21;82(6):658-68. Epub 2011 Jun 21.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bcp.2011.06.017DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3152598PMC
September 2011
6 Reads
24 Citations

Pharmacochemistry of the platelet purinergic receptors.

Purinergic Signal 2011 Sep 18;7(3):305-24. Epub 2011 Feb 18.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bldg. 8A, Rm. B1A-19, NIH, NIDDK, LBC, Bethesda, MD, 20892-0810, USA,

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s11302-011-9216-0DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3166987PMC
September 2011
37 Reads
12 Citations

Allosteric modulation of purine and pyrimidine receptors.

Adv Pharmacol 2011 ;61:187-220

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/B978-0-12-385526-8.00007-2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3165024PMC
August 2011
5 Reads
11 Citations

Pharmacology of purine and pyrimidine receptors. Preface.

Adv Pharmacol 2011 ;61:xv-xvi

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/B978-0-12-385526-8.00020-5DOI Listing
August 2011
3 Reads

Activation of the P2Y1 receptor induces apoptosis and inhibits proliferation of prostate cancer cells.

Biochem Pharmacol 2011 Aug 23;82(4):418-25. Epub 2011 May 23.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bcp.2011.05.013DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3140712PMC
August 2011
28 Reads
14 Citations

Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element.

ACS Med Chem Lett 2011 Aug;2(8):626-631

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/ml200114qDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3156476PMC
August 2011
3 Reads
8 Citations

Striatal adenosine A(2A) receptor-mediated positron emission tomographic imaging in 6-hydroxydopamine-lesioned rats using [(18)F]-MRS5425.

Nucl Med Biol 2011 Aug 30;38(6):897-906. Epub 2011 Mar 30.

Laboratory of Molecular Imaging and Nanomedicine, National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health, Bethesda, MD 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.nucmedbio.2011.01.009DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3157043PMC
August 2011
12 Reads
1 Citation

Predicted structures of agonist and antagonist bound complexes of adenosine A3 receptor.

Proteins 2011 Jun 12;79(6):1878-97. Epub 2011 Apr 12.

Division of Chemistry and Chemical Engineering, Materials and Process Simulation Center MC139-74, California Institute of Technology, Pasadena, California 91125, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1002/prot.23012DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3092833PMC
June 2011
5 Reads
9 Citations

Pyrimidine nucleotides with 4-alkyloxyimino and terminal tetraphosphate δ-ester modifications as selective agonists of the P2Y(4) receptor.

J Med Chem 2011 Jun 20;54(12):4018-33. Epub 2011 May 20.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, Bethesda, Maryland 20892-0810, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm101591jDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3117126PMC
June 2011
9 Reads
12 Citations

Recent developments in adenosine receptor ligands and their potential as novel drugs.

Biochim Biophys Acta 2011 May 23;1808(5):1290-308. Epub 2010 Dec 23.

University of Bonn, An der Immenburg 4, Bonn, Germany.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bbamem.2010.12.017DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3437328PMC
May 2011
2 Reads
72 Citations

Molecular probes for the A2A adenosine receptor based on a pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine scaffold.

Bioorg Med Chem Lett 2011 May 21;21(9):2740-5. Epub 2010 Nov 21.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bldg. 8A, Rm. B1A-19, Bethesda, MD 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2010.11.082DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3081901PMC
May 2011
25 Reads
8 Citations

Comparison of three GPCR structural templates for modeling of the P2Y12 nucleotide receptor.

J Comput Aided Mol Des 2011 Apr 3;25(4):329-38. Epub 2011 Apr 3.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA.

View Article

Download full-text PDF

Source
http://link.springer.com/content/pdf/10.1007/s10822-011-9423
Web Search
http://link.springer.com/10.1007/s10822-011-9423-3
Publisher Site
http://dx.doi.org/10.1007/s10822-011-9423-3DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3157290PMC
April 2011
4 Reads
13 Citations

Structure of an agonist-bound human A2A adenosine receptor.

Science 2011 Apr 10;332(6027):322-7. Epub 2011 Mar 10.

Department of Molecular Biology, Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1126/science.1202793DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3086811PMC
April 2011
15 Reads
276 Citations

International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update.

Pharmacol Rev 2011 Mar 8;63(1):1-34. Epub 2011 Feb 8.

Department of Physiology and Pharmacology, Karolinska Institutet, Stockholm, Sweden.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1124/pr.110.003285DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3061413PMC
March 2011
19 Reads
257 Citations

GPCR ligand-dendrimer (GLiDe) conjugates: Future smart drugs?

Trends in Pharmacological Sciences

View Article
2010
1 Read

Dexamethasone Enhances ATP-Induced Inflammatory Responses in Endothelial Cells

Journal of Pharmacology and Experimental Therapeutics

View Article
2010
1 Read

Adenine nucleotide control of coronary blood flow during exercise

American Journal of Physiology-Heart and Circulatory Physiology

View Article
2010
1 Read

Structure-based Virtual Screening for the discovery of potential P2Y14 receptor ligands

Abstracts of Papers of the American Chemical Society

View Article
2010
1 Read

New frontiers for selective agonists and antagonists of adenosine and P2Y receptors

Abstracts of Papers of the American Chemical Society

View Article
2010
1 Read