Paul G Wyatt

Paul G Wyatt

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Paul G Wyatt

Paul G Wyatt

Publications by authors named "Paul G Wyatt"

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Inhibition of CorA-Dependent Magnesium Homeostasis Is Cidal in Mycobacterium tuberculosis.

Antimicrob Agents Chemother 2019 10 23;63(10). Epub 2019 Sep 23.

Tuberculosis Research Section, Laboratory of Clinical Immunology and Microbiology, National Institute of Allergy and Infectious Disease, National Institutes of Health, Bethesda, Maryland, USA

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http://aac.asm.org/lookup/doi/10.1128/AAC.01006-19
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http://dx.doi.org/10.1128/AAC.01006-19DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6761525PMC
October 2019

Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis.

Proc Natl Acad Sci U S A 2019 04 20;116(14):7015-7020. Epub 2019 Mar 20.

Wellcome Centre for Anti-Infectives Research, Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, University of Dundee, DD1 5EH Dundee, United Kingdom;

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http://www.pnas.org/lookup/doi/10.1073/pnas.1814685116
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http://dx.doi.org/10.1073/pnas.1814685116DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6452685PMC
April 2019

Diversity-oriented synthesis of bicyclic fragments containing privileged azines.

Bioorg Med Chem Lett 2019 01 24;29(2):248-251. Epub 2018 Nov 24.

Drug Discovery Unit, School of Life Sciences, University of Dundee, Dow Street, Dundee DD1 5EH, Scotland, UK. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S0960894X183092
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http://dx.doi.org/10.1016/j.bmcl.2018.11.046DOI Listing
January 2019

Author Correction: Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need.

Nat Rev Microbiol 2018 Nov;16(11):714

Wellcome Centre for Anti-Infectives Research, University of Dundee, Dundee, DD1 5EH, UK.

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http://dx.doi.org/10.1038/s41579-018-0085-1DOI Listing
November 2018

2,4-Diamino-6-methylpyrimidines for the potential treatment of Chagas' disease.

Bioorg Med Chem Lett 2018 10 3;28(18):3025-3030. Epub 2018 Aug 3.

Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee, United Kingdom. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2018.08.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6970618PMC
October 2018

A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors.

J Med Chem 2018 09 12;61(18):8374-8389. Epub 2018 Sep 12.

Drug Discovery Unit, Wellcome Centre for Anti-Infectives Research, Division of Biological Chemistry and Drug Discovery, School of Life Sciences , University of Dundee , Dundee , DD1 5EH , United Kingdom.

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http://dx.doi.org/10.1021/acs.jmedchem.8b00884DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6167002PMC
September 2018

Generation of Polar Semi-Saturated Bicyclic Pyrazoles for Fragment-Based Drug-Discovery Campaigns.

Chemistry 2018 Jul 19;24(41):10443-10451. Epub 2018 Jun 19.

Drug Discovery Unit, School of Life Sciences, University of Dundee, Dow Street, Dundee, DD1 5EH, Scotland, UK.

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http://dx.doi.org/10.1002/chem.201801313DOI Listing
July 2018

Screening a protein kinase inhibitor library against Plasmodium falciparum.

Malar J 2017 11 7;16(1):446. Epub 2017 Nov 7.

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee, DD1 5EH, UK.

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http://dx.doi.org/10.1186/s12936-017-2085-4DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5678585PMC
November 2017

Correction for Arora et al., "Respiratory Flexibility in Response to Inhibition of Cytochrome Oxidase in ".

Antimicrob Agents Chemother 2017 09 24;61(9). Epub 2017 Aug 24.

Tuberculosis Research Section, Laboratory of Clinical Infectious Diseases, National Institute of Allergy and Infectious Disease, National Institutes of Health, Bethesda, Maryland, USA.

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http://dx.doi.org/10.1128/AAC.01429-17DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5571366PMC
September 2017

Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need.

Nat Rev Microbiol 2017 Feb 27;15(4):217-231. Epub 2017 Feb 27.

Wellcome Centre for Anti-Infectives Research, University of Dundee, Dundee DD1 5EH, UK.

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http://dx.doi.org/10.1038/nrmicro.2016.193DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5582623PMC
February 2017

Fragment library design, synthesis and expansion: nurturing a synthesis and training platform.

Drug Discov Today 2017 01 26;22(1):43-56. Epub 2016 Oct 26.

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dow Street, Dundee, DD1 5EH, Scotland, UK. Electronic address:

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http://dx.doi.org/10.1016/j.drudis.2016.10.005DOI Listing
January 2017

Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei.

J Med Chem 2015 Oct 29;58(19):7695-706. Epub 2015 Sep 29.

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee, DD1 5EH, U.K.

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http://dx.doi.org/10.1021/acs.jmedchem.5b00596DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4601051PMC
October 2015

N-myristoyltransferase is a cell wall target in Aspergillus fumigatus.

ACS Chem Biol 2015 Jun 27;10(6):1425-34. Epub 2015 Feb 27.

†Division of Molecular Microbiology, ‡Division of Biological Chemistry and Drug Discovery, §MRC Protein Phosphorylation and Ubiquitylation Unit, College of Life Sciences, University of Dundee, Dundee, DD1 5EH, United Kingdom.

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http://dx.doi.org/10.1021/cb5008647DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4477619PMC
June 2015

Identification and structure solution of fragment hits against kinetoplastid N-myristoyltransferase.

Acta Crystallogr F Struct Biol Commun 2015 May 21;71(Pt 5):586-93. Epub 2015 Apr 21.

Drug Discovery Unit, College of Life Sciences, University of Dundee, Dow Street, Dundee DD1 5EH, Scotland.

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http://dx.doi.org/10.1107/S2053230X15003040DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4427169PMC
May 2015

Respiratory flexibility in response to inhibition of cytochrome C oxidase in Mycobacterium tuberculosis.

Antimicrob Agents Chemother 2014 Nov 25;58(11):6962-5. Epub 2014 Aug 25.

Tuberculosis Research Section, Laboratory of Clinical Infectious Diseases, National Institute of Allergy and Infectious Disease, National Institutes of Health, Bethesda, Maryland, USA

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http://dx.doi.org/10.1128/AAC.03486-14DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4249445PMC
November 2014

Clinically relevant enhancement of human sperm motility using compounds with reported phosphodiesterase inhibitor activity.

Hum Reprod 2014 Oct 14;29(10):2123-35. Epub 2014 Aug 14.

Reproductive and Developmental Biology, Medical School, Ninewells Hospital, University of Dundee, Dundee DD1 9SY, UK Assisted Conception Unit, NHS Tayside, Ninewells Hospital, Dundee DD1 9SY, UK.

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http://dx.doi.org/10.1093/humrep/deu196DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4481575PMC
October 2014

A target repurposing approach identifies N-myristoyltransferase as a new candidate drug target in filarial nematodes.

PLoS Negl Trop Dis 2014 Sep 4;8(9):e3145. Epub 2014 Sep 4.

New England Biolabs, Division of Genome Biology, Ipswich, Massachusetts, United States of America.

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http://dx.doi.org/10.1371/journal.pntd.0003145DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4154664PMC
September 2014

The design and synthesis of potent and selective inhibitors of Trypanosoma brucei glycogen synthase kinase 3 for the treatment of human african trypanosomiasis.

J Med Chem 2014 Sep 8;57(18):7536-49. Epub 2014 Sep 8.

Drug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dow Street, Dundee DD1 5EH, U.K.

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http://dx.doi.org/10.1021/jm500239bDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4175002PMC
September 2014

Exploring the Trypanosoma brucei Hsp83 potential as a target for structure guided drug design.

PLoS Negl Trop Dis 2013 17;7(10):e2492. Epub 2013 Oct 17.

The Structural Genomics Consortium (SGC), University of Toronto, Toronto, Ontario, Canada ; Department of Tropical Medicine, School of Public Health and Tropical Medicine, Tulane University, New Orleans, Louisiana, United States of America.

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http://www.drugdiscovery.dundee.ac.uk/sites/www.drugdiscover
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http://dx.plos.org/10.1371/journal.pntd.0002492
Publisher Site
http://dx.doi.org/10.1371/journal.pntd.0002492DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3798429PMC
May 2014

Fragment-based hit identification: thinking in 3D.

Drug Discov Today 2013 Dec 30;18(23-24):1221-7. Epub 2013 Jul 30.

College of Life Sciences, Sir James Black Centre, University of Dundee, Dundee DD1 5EH, UK. Electronic address:

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http://dx.doi.org/10.1016/j.drudis.2013.07.011DOI Listing
December 2013

Structure-activity relationship studies of pyrrolone antimalarial agents.

ChemMedChem 2013 Sep 5;8(9):1537-44. Epub 2013 Aug 5.

Division of Biological Chemistry & Drug Discovery, College of Life Sciences, University of Dundee, Sir James Black Centre, Dow St, Dundee DD1 5EH, UK.

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http://dx.doi.org/10.1002/cmdc.201300177DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3963473PMC
September 2013

Comparison of a high-throughput high-content intracellular Leishmania donovani assay with an axenic amastigote assay.

Antimicrob Agents Chemother 2013 Jul 9;57(7):2913-22. Epub 2013 Apr 9.

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, University of Dundee, Dundee, United Kingdom.

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http://dx.doi.org/10.1128/AAC.02398-12DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3697379PMC
July 2013

From on-target to off-target activity: identification and optimisation of Trypanosoma brucei GSK3 inhibitors and their characterisation as anti-Trypanosoma brucei drug discovery lead molecules.

ChemMedChem 2013 Jul 14;8(7):1127-37. Epub 2013 Jun 14.

Drug Discovery Unit (DDU), Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Sir James Black Centre, DD1 5EH, UK.

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http://dx.doi.org/10.1002/cmdc.201300072DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3728731PMC
July 2013

De novo design of protein kinase inhibitors by in silico identification of hinge region-binding fragments.

ACS Chem Biol 2013 May 27;8(5):1044-52. Epub 2013 Mar 27.

Drug Discovery Unit (DDU), Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Sir James Black Centre, DD1 5EH, UK.

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http://pubs.acs.org/doi/10.1021/cb300729y
Publisher Site
http://dx.doi.org/10.1021/cb300729yDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3833278PMC
May 2013

Quinol derivatives as potential trypanocidal agents.

Bioorg Med Chem 2012 Feb 27;20(4):1607-15. Epub 2011 Dec 27.

Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, UK.

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http://dx.doi.org/10.1016/j.bmc.2011.12.018DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3281193PMC
February 2012

Design, synthesis and biological evaluation of Trypanosoma brucei trypanothione synthetase inhibitors.

ChemMedChem 2012 Jan 8;7(1):95-106. Epub 2011 Dec 8.

Drug Discovery Unit, Division of Biological Chemistry & Drug Discovery, College of Life Sciences, University of Dundee, Dundee, UK.

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http://dx.doi.org/10.1002/cmdc.201100420DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3320663PMC
January 2012

Identification of inhibitors of the Leishmania cdc2-related protein kinase CRK3.

ChemMedChem 2011 Dec 13;6(12):2214-24. Epub 2011 Sep 13.

Drug Discovery Unit, College of Life Sciences, James Black Centre, University of Dundee, Dundee, DD1 5EH, UK.

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http://dx.doi.org/10.1002/cmdc.201100344DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3272345PMC
December 2011

Optimisation of the anti-Trypanosoma brucei activity of the opioid agonist U50488.

ChemMedChem 2011 Oct 10;6(10):1832-40. Epub 2011 Aug 10.

Drug Discovery Unit, College of Life Sciences, James Black Centre, University of Dundee, Dundee, DD1 5EH, Scotland, UK.

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http://dx.doi.org/10.1002/cmdc.201100278DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3229842PMC
October 2011

Target validation: linking target and chemical properties to desired product profile.

Curr Top Med Chem 2011 ;11(10):1275-83

Drug Discovery Unit, College of Life Sciences, University of Dundee, UK.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3182078PMC
http://dx.doi.org/10.2174/156802611795429185DOI Listing
August 2011

Progress in neglected disease drug discovery.

Curr Top Med Chem 2011 ;11(10):1215

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http://dx.doi.org/10.2174/156802611795429149DOI Listing
August 2011

Antitumor quinol PMX464 is a cytocidal anti-trypanosomal inhibitor targeting trypanothione metabolism.

J Biol Chem 2011 Mar 6;286(10):8523-33. Epub 2011 Jan 6.

Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, United Kingdom.

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http://dx.doi.org/10.1074/jbc.M110.214833DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3048735PMC
March 2011

Design, synthesis and biological evaluation of novel inhibitors of Trypanosoma brucei pteridine reductase 1.

ChemMedChem 2011 Feb 29;6(2):302-8. Epub 2010 Dec 29.

Drug Discovery Unit, Division of Biological Chemistry & Drug Discovery, College of Life Sciences, University of Dundee, Sir James Black Centre, Dundee, Scotland, DD1 5EH, UK.

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http://dx.doi.org/10.1002/cmdc.201000450DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3047710PMC
February 2011

Chemical validation of trypanothione synthetase: a potential drug target for human trypanosomiasis.

J Biol Chem 2009 Dec 14;284(52):36137-45. Epub 2009 Oct 14.

Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, Scotland, United Kingdom.

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http://dx.doi.org/10.1074/jbc.M109.045336DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2794729PMC
December 2009

Investigation of trypanothione reductase as a drug target in Trypanosoma brucei.

ChemMedChem 2009 Dec;4(12):2060-9

Drug Discovery Unit, College of Life Sciences, University of Dundee, Sir James Black Centre, Dundee, DD1 5EH, UK.

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http://dx.doi.org/10.1002/cmdc.200900262DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2855869PMC
December 2009

The emerging academic drug-discovery sector.

Authors:
Paul G Wyatt

Future Med Chem 2009 Sep;1(6):1013-7

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http://dx.doi.org/10.4155/fmc.09.78DOI Listing
September 2009

Synthesis and evaluation of 1-(1-(Benzo[b]thiophen-2-yl)cyclohexyl)piperidine (BTCP) analogues as inhibitors of trypanothione reductase.

ChemMedChem 2009 Aug;4(8):1341-53

Division of Biological Chemistry & Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, UK.

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http://dx.doi.org/10.1002/cmdc.200900098DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2929374PMC
August 2009

Target assessment for antiparasitic drug discovery.

Trends Parasitol 2007 Dec 24;23(12):589-95. Epub 2007 Oct 24.

Drug Discovery Unit, College of Life Sciences, University of Dundee, Dundee DD1 5EH, UK.

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http://dx.doi.org/10.1016/j.pt.2007.08.019DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2979298PMC
December 2007

2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 2. Synthesis, chirality, and pharmacokinetics.

J Med Chem 2005 Nov;48(22):6956-69

Department of Medicinal Chemistry, GlaxoSmithKline Research and Development, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts SG1 2NY, U.K.

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http://dx.doi.org/10.1021/jm050557vDOI Listing
November 2005

2,5-Diketopiperazines as potent and selective oxytocin antagonists 1: Identification, stereochemistry and initial SAR.

Bioorg Med Chem Lett 2005 May;15(10):2579-82

Department of Medicinal Chemistry CVU UK, GlaxoSmithKline Research and Development Limited, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts SG1 2NY, UK.

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http://dx.doi.org/10.1016/j.bmcl.2005.03.045DOI Listing
May 2005

Detection of ligands from a dynamic combinatorial library by X-ray crystallography.

Angew Chem Int Ed Engl 2003 Sep;42(37):4479-82

Astex Technology, 436 Cambridge Science Park, Milton Road, Cambridge CB4 0QA, UK.

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http://dx.doi.org/10.1002/anie.200351951DOI Listing
September 2003

Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives.

Bioorg Med Chem Lett 2002 May;12(10):1399-404

Department of Medicinal Chemistry, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, SG1 2NY, Herts, UK.

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http://dx.doi.org/10.1016/s0960-894x(02)00159-2DOI Listing
May 2002

Enantioselective Recognition of Amino Acids by Axially-Chiral pi-Electron-Deficient Receptors.

J Org Chem 1996 Oct;61(21):7234-7235

School of Chemistry, University of Birmingham, Edgbaston, Birmingham B15 2TT, U.K., and Glaxo Wellcome Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.

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http://dx.doi.org/10.1021/jo961256jDOI Listing
October 1996