Richard A Houghten

Richard A Houghten

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Richard A Houghten

Publications by authors named "Richard A Houghten"

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Exploring the chemical space of peptides for drug discovery: a focus on linear and cyclic penta-peptides.

Mol Divers 2018 May 14;22(2):259-267. Epub 2018 Feb 14.

School of Chemistry, Department of Pharmacy, Universidad Nacional Autónoma de México, Avenida Universidad 3000, 04510, Mexico City, Mexico.

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http://dx.doi.org/10.1007/s11030-018-9812-9DOI Listing
May 2018

Mu-Opioid receptor biased ligands: A safer and painless discovery of analgesics?

Drug Discov Today 2017 11 22;22(11):1719-1729. Epub 2017 Jul 22.

Instituto de Química, Universidad Nacional Autónoma de México, Av. Universidad 3000, Mexico City 04510, Mexico. Electronic address:

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http://dx.doi.org/10.1016/j.drudis.2017.07.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6620030PMC
November 2017

A one-pot multicomponent approach to a new series of morphine derivatives and their biological evaluation.

Org Biomol Chem 2017 Sep;15(37):7796-7801

Department of Chemistry, Zhejiang Sci-Tech University, Hangzhou, Zhejiang 310018, P. R. China.

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http://dx.doi.org/10.1039/c7ob01924fDOI Listing
September 2017

Identification of a Hit Series of Antileishmanial Compounds through the Use of Mixture-Based Libraries.

ACS Med Chem Lett 2017 Aug 10;8(8):802-807. Epub 2017 Jul 10.

Department of Chemistry, University of South Florida, CHE 205, 4202 East Fowler Avenue, Tampa, Florida 33620, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.7b00045DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5554901PMC
August 2017

Identification of 5,6-dihydroimidazo[2,1-b]thiazoles as a new class of antimicrobial agents.

Bioorg Med Chem 2016 11 12;24(21):5633-5638. Epub 2016 Sep 12.

Department of Cell Biology, Microbiology and Molecular Biology, University of South Florida, 4202 East Fowler Avenue, Tampa, FL 33620, United States.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5065789PMC
http://dx.doi.org/10.1016/j.bmc.2016.09.027DOI Listing
November 2016

Small-Molecule Inhibitors Targeting Topoisomerase I as Novel Antituberculosis Agents.

Antimicrob Agents Chemother 2016 07 20;60(7):4028-36. Epub 2016 Jun 20.

Department of Chemistry and Biochemistry, Florida International University, Miami, Florida, USA Biomolecular Sciences Institute, Florida International University, Miami, Florida, USA

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http://dx.doi.org/10.1128/AAC.00288-16DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4914652PMC
July 2016

Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.

J Med Chem 2016 Feb 29;59(3):1239-45. Epub 2016 Jan 29.

Torrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.5b01899DOI Listing
February 2016

Identification of Small Molecule Inhibitors of Human As(III) S-Adenosylmethionine Methyltransferase (AS3MT).

Chem Res Toxicol 2015 Dec 6;28(12):2419-25. Epub 2015 Dec 6.

Department of Cellular Biology and Pharmacology, Herbert Wertheim College of Medicine, Florida International University , Miami, Florida 33199, United States.

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http://dx.doi.org/10.1021/acs.chemrestox.5b00432DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4688878PMC
December 2015

Parallel Synthesis of Hexahydrodiimidazodiazepines Heterocyclic Peptidomimetics and Their in Vitro and in Vivo Activities at μ (MOR), δ (DOR), and κ (KOR) Opioid Receptors.

J Med Chem 2015 Jun 4;58(12):4905-17. Epub 2015 Jun 4.

Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.

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http://dx.doi.org/10.1021/jm501637cDOI Listing
June 2015

Combinatorial Libraries As a Tool for the Discovery of Novel, Broad-Spectrum Antibacterial Agents Targeting the ESKAPE Pathogens.

J Med Chem 2015 Apr 1;58(8):3340-55. Epub 2015 Apr 1.

∥Torrey Pines Institute for Molecular Studies, Port St. Lucie, Florida 34987, United States.

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http://dx.doi.org/10.1021/jm501628sDOI Listing
April 2015

Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities.

Eur J Med Chem 2015 Mar 29;92:270-81. Epub 2014 Dec 29.

Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China; Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie, FL 34987, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2014.12.049DOI Listing
March 2015

Discovery of a potent and selective α3β4 nicotinic acetylcholine receptor antagonist from an α-conotoxin synthetic combinatorial library.

J Med Chem 2014 Apr 3;57(8):3511-21. Epub 2014 Apr 3.

Torrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.

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http://dx.doi.org/10.1021/jm500183rDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4358631PMC
April 2014

Glycosylation of a disintegrin and metalloprotease 17 affects its activity and inhibition.

Anal Biochem 2014 Mar 19;449:68-75. Epub 2013 Dec 19.

Torrey Pines Institute for Molecular Studies, Port St. Lucie, FL 34987, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ab.2013.12.018DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4334441PMC
March 2014

Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis.

J Med Chem 2014 Feb 5;57(4):1599-608. Epub 2014 Feb 5.

Torrey Pines Institute for Molecular Studies , 11350 South West Village Parkway, Port St. Lucie, Florida 34987, United States.

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http://dx.doi.org/10.1021/jm4019542DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3983399PMC
February 2014

Scaffold ranking and positional scanning utilized in the discovery of nAChR-selective compounds suitable for optimization studies.

J Med Chem 2013 Dec 12;56(24):10103-17. Epub 2013 Dec 12.

Torrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.

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http://dx.doi.org/10.1021/jm401543hDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4106133PMC
December 2013

Dissociation of antimicrobial and hemolytic activities of gramicidin S through N-methylation modification.

ChemMedChem 2013 Nov 10;8(11):1865-72. Epub 2013 Sep 10.

Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port Saint Lucie, FL 34987 (USA).

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http://doi.wiley.com/10.1002/cmdc.201300232
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http://dx.doi.org/10.1002/cmdc.201300232DOI Listing
November 2013

Conditional probabilistic analysis for prediction of the activity landscape and relative compound activities.

J Chem Inf Model 2013 Oct 17;53(10):2613-25. Epub 2013 Sep 17.

Torrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.

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http://dx.doi.org/10.1021/ci400243eDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3850180PMC
October 2013

Ligand/kappa-opioid receptor interactions: insights from the X-ray crystal structure.

Eur J Med Chem 2013 Aug 30;66:114-21. Epub 2013 May 30.

Instituto de Química, UNAM, Av. Universidad 3000, México DF, Mexico.

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http://dx.doi.org/10.1016/j.ejmech.2013.05.021DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3775475PMC
August 2013

Libraries from Libraries: A Series of Sulfonamide Linked Heterocycles Derived from the Same Scaffold.

Tetrahedron Lett 2013 Aug;54(32)

Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie FL 34987.

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http://dx.doi.org/10.1016/j.tetlet.2013.06.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3867824PMC
August 2013

Parallel synthesis of 1,6-disubstituted-1,2,4-triazin-3-ones on solid-phase.

ACS Comb Sci 2013 Jul 13;15(7):335-9. Epub 2013 Jun 13.

Institute of Materia Medica, College of Pharmaceutical Sciences, Zhejiang University , Hangzhou 310058, P.R. China.

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http://dx.doi.org/10.1021/co400064dDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3875618PMC
July 2013

Shifting from the single to the multitarget paradigm in drug discovery.

Drug Discov Today 2013 May 20;18(9-10):495-501. Epub 2013 Jan 20.

Instituto de Química, Universidad Nacional Autónoma de México, Circuito Exterior, Ciudad Universitaria, México, D.F. 04510, Mexico.

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http://dx.doi.org/10.1016/j.drudis.2013.01.008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3642214PMC
May 2013

The role of imidazole in peptide cyclization by transesterification: parallels to the catalytic triads of serine proteases.

Org Biomol Chem 2013 May;11(18):2979-87

Torrey Pines Institute for Molecular Studies, 11350 Southwest Village Parkway, Port St. Lucie, FL 34987, USA.

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http://dx.doi.org/10.1039/c3ob27464kDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4106122PMC
May 2013

Fluorescent mu selective opioid ligands from a mixture based cyclic peptide library.

ACS Comb Sci 2012 Dec 8;14(12):673-9. Epub 2012 Nov 8.

Torrey Pines Institute for Molecular Studies, Port Saint Lucie, Florida 34987, United States.

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http://pubs.acs.org/doi/10.1021/co300110t
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http://dx.doi.org/10.1021/co300110tDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3607207PMC
December 2012

The Multi-Leu peptide inhibitor discriminates between PACE4 and furin and exhibits antiproliferative effects on prostate cancer cells.

J Med Chem 2012 Dec 14;55(23):10501-11. Epub 2012 Nov 14.

Institut de Pharmacologie de Sherbrooke, Département de Chirurgie/Urologie, Faculté de Médecine et des Sciences de la Santé, Université de Sherbrooke, 3001 12e Avenue Nord, Sherbrooke, Québec J1H 5N4, Canada.

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http://dx.doi.org/10.1021/jm3011178DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3523546PMC
December 2012

Palladium-catalyzed C-H functionalization using guanidine as a directing group: ortho arylation and olefination of arylguanidines.

Org Lett 2012 Nov 24;14(21):5452-5. Epub 2012 Oct 24.

Institute of Materia Medica, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, P. R. China.

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http://dx.doi.org/10.1021/ol302533wDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3786205PMC
November 2012

Identification of B cell and T cell epitopes using synthetic peptide combinatorial libraries.

Curr Protoc Immunol 2012 Nov;Chapter 9:Unit9.5

Torrey Pines Institute for Molecular Studies, San Diego, CA, USA.

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http://dx.doi.org/10.1002/0471142735.im0905s99DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3511046PMC
November 2012

A novel method for the determination of isokinetic ratios and its application in the synthesis of two new positional scanning libraries.

ACS Comb Sci 2012 Sep 28;14(9):503-12. Epub 2012 Aug 28.

Torrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.

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http://dx.doi.org/10.1021/co300060sDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3825827PMC
September 2012

Expanding the medicinally relevant chemical space with compound libraries.

Drug Discov Today 2012 Jul 10;17(13-14):718-26. Epub 2012 Apr 10.

Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie, FL 34987, USA.

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http://dx.doi.org/10.1016/j.drudis.2012.04.001DOI Listing
July 2012

Multitarget structure-activity relationships characterized by activity-difference maps and consensus similarity measure.

J Chem Inf Model 2011 Sep 29;51(9):2427-39. Epub 2011 Aug 29.

Torrey Pines Institute for Molecular Studies, Port St. Lucie, Florida 34987, United States.

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http://dx.doi.org/10.1021/ci200281vDOI Listing
September 2011

Integrating virtual screening and combinatorial chemistry for accelerated drug discovery.

Comb Chem High Throughput Screen 2011 Jul;14(6):475-87

Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie, FL 34987, USA.

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http://dx.doi.org/10.2174/138620711795767866DOI Listing
July 2011

Integrating computational and mixture-based screening of combinatorial libraries.

J Mol Model 2011 Jun 21;17(6):1473-82. Epub 2010 Sep 21.

Torrey Pines Institute for Molecular Studies, Port St Lucie, FL 34987, USA.

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http://dx.doi.org/10.1007/s00894-010-0850-1DOI Listing
June 2011

Increased diversity of libraries from libraries: chemoinformatic analysis of bis-diazacyclic libraries.

Chem Biol Drug Des 2011 May 1;77(5):328-42. Epub 2011 Mar 1.

Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie, FL 34987, USA.

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http://dx.doi.org/10.1111/j.1747-0285.2011.01100.xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3077462PMC
May 2011

Use and implications of the harmonic mean model on mixtures for basic research and drug discovery.

ACS Comb Sci 2011 May 11;13(3):337-44. Epub 2011 Mar 11.

Torrey Pines Institute for Molecular Studies , Port St. Lucie, Florida 34987, United States.

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http://dx.doi.org/10.1021/co100065aDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3096014PMC
May 2011

High Throughput Synthesis of 2,3,6-Trisubstituted-5,6-Dihydroimidazo[2,1-b]thiazole Derivatives.

Tetrahedron Lett 2011 Feb;52(6):696-698

Torrey Pines Institute for Molecular Studies, 11350 Village Parkway, Port St. Lucie, FL 34987.

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http://dx.doi.org/10.1016/j.tetlet.2010.12.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3065664PMC
February 2011

A Facile Approach to the Synthesis of 3,4-Disubstituted-2-Aminothiazolium Derivatives through the Use of A "Volatilizable" Support.

Tetrahedron Lett 2010 Oct;51(43):5637-5639

Torrey Pines Institute for Molecular Studies, 11350 Village Parkway, Port St. Lucie, FL 34987.

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http://dx.doi.org/10.1016/j.tetlet.2010.08.026DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3133972PMC
October 2010

Macrolactonization of peptide thioesters catalyzed by imidazole and its application in the synthesis of kahalalide B and analogues.

Org Lett 2010 May;12(10):2250-3

Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie, Florida 34987, USA.

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http://dx.doi.org/10.1021/ol100596pDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3118573PMC
May 2010

Conformational landscape of platinum(II)-tetraamine complexes: DFT and NBO studies.

J Comput Aided Mol Des 2010 Mar 24;24(3):225-35. Epub 2010 Mar 24.

Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie, FL 34987, USA.

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http://dx.doi.org/10.1007/s10822-010-9328-6DOI Listing
March 2010

Synthesis of cyclic peptides through direct aminolysis of peptide thioesters catalyzed by imidazole in aqueous organic solutions.

J Comb Chem 2009 Nov-Dec;11(6):1066-72

Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port Saint Lucie, Florida 34987, USA.

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http://dx.doi.org/10.1021/cc900100zDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3121167PMC
February 2010

Modeling of peptides containing D-amino acids: implications on cyclization.

J Comput Aided Mol Des 2009 Sep 11;23(9):677-89. Epub 2009 Jul 11.

Torrey Pines Institute for Molecular Studies, Port Saint Lucie, FL 34987, USA.

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http://dx.doi.org/10.1007/s10822-009-9295-yDOI Listing
September 2009

Parallel synthesis of chiral pentaamines and pyrrolidine containing bis-heterocyclic libraries. Multiple scaffolds with multiple building blocks: a double diversity for the identification of new antitubercular compounds.

Bioorg Med Chem Lett 2009 Sep 9;19(17):5169-75. Epub 2009 Jul 9.

Torrey Pines Institute for Molecular Studies, 3550 Genearl Atomocs Court, San Diego, CA 92121, USA.

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http://dx.doi.org/10.1016/j.bmcl.2009.07.010DOI Listing
September 2009

Identification, structure-activity relationships and molecular modeling of potent triamine and piperazine opioid ligands.

Bioorg Med Chem 2009 Aug 21;17(15):5583-97. Epub 2009 Jun 21.

Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Room 132, Port St. Lucie, FL 34987, USA.

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http://dx.doi.org/10.1016/j.bmc.2009.06.026DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2746904PMC
August 2009

Chemoinformatic analysis of combinatorial libraries, drugs, natural products, and molecular libraries small molecule repository.

J Chem Inf Model 2009 Apr;49(4):1010-24

Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie, Florida 34987, USA.

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http://dx.doi.org/10.1021/ci800426uDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2686115PMC
April 2009

Synthetic small-molecule prohormone convertase 2 inhibitors.

Mol Pharmacol 2009 Mar 12;75(3):617-25. Epub 2008 Dec 12.

Department of Anatomy and Neurobiology, University of Maryland at Baltimore, Baltimore, Maryland 21201, USA.

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http://dx.doi.org/10.1124/mol.108.051334DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2684913PMC
March 2009

One-pot high-throughput synthesis of beta-turn cyclic peptidomimetics via "volatilizable" supports.

J Org Chem 2009 Mar;74(5):2183-5

Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port Saint Lucie, Florida 34987, USA.

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http://dx.doi.org/10.1021/jo802583tDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3117271PMC
March 2009

Characterization of activity landscapes using 2D and 3D similarity methods: consensus activity cliffs.

J Chem Inf Model 2009 Feb;49(2):477-91

Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie, Florida 34987, USA.

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http://pubs.acs.org/doi/abs/10.1021/ci800379q
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http://dx.doi.org/10.1021/ci800379qDOI Listing
February 2009

From rapid in vitro screening to rapid in vivo screening in the drug discovery process.

Neuropsychopharmacology 2009 Jan;34(1):251-2

Center for Organic and Medicinal Chemistry, Research Triangle Institute, Research Triangle Park, NC, USA.

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http://dx.doi.org/10.1038/npp.2008.160DOI Listing
January 2009

High throughput synthesis of peptide alpha-thioesters through the use of "volatilizable" support.

J Comb Chem 2008 Sep-Oct;10(5):613-6. Epub 2008 Aug 19.

College of Pharmaceutical Science, Zhejiang University, Hangzhou, P. R. China.

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http://dx.doi.org/10.1021/cc800076bDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3117248PMC
November 2008

Solid-phase synthesis of 4,8-disubstituted-8,9-dihydropyrazino[2,3-g]quinazolin-7(6H)-ones.

Biopolymers 2008 ;90(3):439-43

College of Pharmaceutical Science, Zhejiang University, Zijin Campus, Hangzhou 310058, People's Republic of China.

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http://dx.doi.org/10.1002/bip.20842DOI Listing
July 2008

Conformation-opioid activity relationships of bicyclic guanidines from 3D similarity analysis.

Bioorg Med Chem 2008 Jun 27;16(11):5932-8. Epub 2008 Apr 27.

Torrey Pines Institute for Molecular Studies, 5775 Old Dixie Highway, Fort Pierce, FL 34946, USA.

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http://dx.doi.org/10.1016/j.bmc.2008.04.061DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2533277PMC
June 2008

A similarity-based data-fusion approach to the visual characterization and comparison of compound databases.

Chem Biol Drug Des 2007 Nov 10;70(5):393-412. Epub 2007 Oct 10.

College of Pharmacy & BIO5 Institute, University of Arizona, Tucson, AZ 85721, USA.

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http://dx.doi.org/10.1111/j.1747-0285.2007.00579.xDOI Listing
November 2007

A traceless approach for the solid-phase parallel synthesis of trisubstituted oxindoles.

J Comb Chem 2007 Jul-Aug;9(4):566-8. Epub 2007 May 12.

Department of Medicinal Chemistry, College of Pharmaceutical Sciences, Zijin Campus, Zhejiang University, Hangzhou, Zhejiang 310058, P. R. China.

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http://dx.doi.org/10.1021/cc070010xDOI Listing
August 2007

Scaffold approach for solid-phase synthesis of 2,3-disubstituted 8-arylamino-3H-imidazo[4,5-g]quinazolines.

J Comb Chem 2007 Jan-Feb;9(1):9-11

College of Pharmaceutical Science, Zijin Campus, Zhejiang University, Hangzhou 310058, P.R. China.

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http://dx.doi.org/10.1021/cc0601231DOI Listing
March 2007

Short polybasic peptide sequences are potent inhibitors of PC5/6 and PC7: Use of positional scanning-synthetic peptide combinatorial libraries as a tool for the optimization of inhibitory sequences.

Mol Pharmacol 2007 Jan 29;71(1):323-32. Epub 2006 Sep 29.

Département de Pharmacologie, Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke, 3001, 12 Ave. Nord., Sherbrooke, Québec, Canada J1H 5N4.

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http://dx.doi.org/10.1124/mol.106.027946DOI Listing
January 2007

Synthesis of platinum(II) chiral tetraamine coordination complexes.

J Comb Chem 2006 Sep-Oct;8(5):780-3

Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, California 92121, USA.

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http://dx.doi.org/10.1021/cc060045hDOI Listing
November 2006

Identification of potent and highly selective chiral tri-amine and tetra-amine mu opioid receptors ligands: an example of lead optimization using mixture-based libraries.

Bioorg Med Chem Lett 2006 Aug 5;16(16):4331-8. Epub 2006 Jun 5.

Torrey Pines Institute for Molecular Studies, San Diego, CA 92121, USA.

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http://dx.doi.org/10.1016/j.bmcl.2006.05.053DOI Listing
August 2006

In vitro and direct in vivo testing of mixture-based combinatorial libraries for the identification of highly active and specific opiate ligands.

AAPS J 2006 May 26;8(2):E371-82. Epub 2006 May 26.

Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, CA 92121, USA.

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http://dx.doi.org/10.1007/BF02854908DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3231577PMC
May 2006

Solid phase synthesis of 3,4,7-trisubstituted 4,5,8,9-tetrahydro-3H-imidazo[1,2-a][1,3,5]triazepin-2(7H)-thiones and N-alkyl-4,5,7,8-tetrahydro-3H-imidazo[1,2-a][1,3,5]triazepin-2-amines.

J Comb Chem 2006 Jan-Feb;8(1):127-31

Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, California 92121, USA.

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http://dx.doi.org/10.1021/cc050094eDOI Listing
February 2006

"Volatilizable" supports for high-throughput organic synthesis.

J Am Chem Soc 2005 Jun;127(24):8582-3

Torrey Pines Institute for Molecular Studies and Mixture Sciences Inc., 3550 General Atomics Court, San Diego, California 92121, USA.

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http://dx.doi.org/10.1021/ja0402396DOI Listing
June 2005

Improved, high yield synthesis of 3H-quinazolin-4-ones, the key intermediates of recently developed drugs.

Curr Med Chem 2004 Oct;11(19):2549-53

Department of Pharmaceutical Chemistry, Semmelweis University, Högyes E. u. 9, Budapest, Hungary.

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http://dx.doi.org/10.2174/0929867043364423DOI Listing
October 2004

Inhibition of furin by polyarginine-containing peptides: nanomolar inhibition by nona-D-arginine.

J Biol Chem 2004 Aug 14;279(35):36788-94. Epub 2004 Jun 14.

Department of Biochemistry and Molecular Biology, Louisiana State University Health Sciences Center, 1901 Perdido Street, New Orleans, LA 70112, USA.

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http://dx.doi.org/10.1074/jbc.M400484200DOI Listing
August 2004

A traceless approach for the solid-phase synthesis of 6-amino-1,3,5-triazine-2,4-diones.

J Comb Chem 2004 Jan-Feb;6(1):83-5

Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, California 92121, USA.

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http://dx.doi.org/10.1021/cc030017oDOI Listing
June 2004

Halogenoalkyl isocyanates as bifunctional reagents in an Aza-Wittig/heterocyclization reaction on the solid phase: efficient entry into new tetracyclic benzimidazole systems.

J Comb Chem 2004 Mar-Apr;6(2):220-3

Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, CA 92121, USA.

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http://dx.doi.org/10.1021/cc030036yDOI Listing
May 2004

De novo identification of highly active fluorescent kappa opioid ligands from a rhodamine labeled tetrapeptide positional scanning library.

Bioorg Med Chem Lett 2004 Apr;14(8):1947-51

Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, CA 92121, USA.

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http://dx.doi.org/10.1016/j.bmcl.2004.01.090DOI Listing
April 2004

Mixture-based combinatorial libraries: from peptides and peptidomimetics to small molecule acyclic and heterocyclic compounds.

Methods Enzymol 2003 ;369:496-517

Torrey Pines Institute, Room 2-136, 3550 General Atomics Court, San Diego, California 92121, USA.

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http://dx.doi.org/10.1016/S0076-6879(03)69025-7DOI Listing
February 2004

Specificity and degeneracy of T cells.

Mol Immunol 2004 Feb;40(14-15):1047-55

Torrey Pines Institute for Molecular Studies, San Diego, CA 92121, USA.

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http://dx.doi.org/10.1016/j.molimm.2003.11.022DOI Listing
February 2004

Peptidic complex mixtures as therapeutic agents in CNS autoimmunity.

Mol Immunol 2004 Feb;40(14-15):1075-87

NINDS, NIH, Building 10, Room 5B16, 10 Center Drive MSC 1400, Bethesda, MD 20892, USA.

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http://dx.doi.org/10.1016/j.molimm.2003.11.006DOI Listing
February 2004

Parallel solid-phase synthesis of 2-imino-4-oxo-1,3,5-triazino[1,2-a]benzimidazoles via tandem aza-Wittig/heterocumulene-mediated annulation reaction.

J Comb Chem 2003 Mar-Apr;5(2):155-60

Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, California 92121, USA.

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http://dx.doi.org/10.1021/cc020077eDOI Listing
May 2003

Combinatorial chemistry: mixture-based combinatorial libraries of acyclic and heterocyclic compounds from amino acids and short peptides.

EXS 2003 (93):109-23

Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, CA 92121, USA.

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http://dx.doi.org/10.1007/978-3-0348-7997-2_6DOI Listing
April 2003

Parallel solid-phase synthesis of disubstituted 1,6-piperazine-2-ones.

J Comb Chem 2002 Nov-Dec;4(6):542-5

Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, California 92121, USA.

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http://dx.doi.org/10.1021/cc0200235DOI Listing
January 2003

Advances in the use of synthetic combinatorial chemistry: mixture-based libraries.

Nat Med 2003 Jan;9(1):118-22

Torrey Pines Institute for Molecular Studies, San Diego, California, USA.

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http://dx.doi.org/10.1038/nm0103-118DOI Listing
January 2003

The combined solid/solution-phase synthesis of nitrosamines: the evolution of the "libraries from libraries" concept.

J Org Chem 2003 Jan;68(1):183-6

Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, California 92121, USA.

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http://dx.doi.org/10.1021/jo0204909DOI Listing
January 2003

Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin.

Bioorg Med Chem Lett 2002 Nov;12(21):3175-8

Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, CA 92121, USA.

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http://dx.doi.org/10.1016/s0960-894x(02)00678-9DOI Listing
November 2002

Use of Vilsmeier reagent for the solid-phase synthesis of 1,5-disubstituted 4,5-dihydro-1H-imidazoles and disubstituted 4,5-dihydro-1H-imidazolylbenzimidazoles.

J Comb Chem 2002 Sep-Oct;4(5):496-500

Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, CA 92121, USA.

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http://dx.doi.org/10.1021/cc020020sDOI Listing
October 2002