Paul G Wyatt (0000-0002-0397-245X)

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Biography

Paul is currently Head of The Drug Discovery Unit. His current role is to develop translational research at Dundee, by bringing together his and other’s experience of Drug Discovery in the Pharma/Biotech sector with basic academic research to de-risk novel targets for drug discovery and new treatments for diseases such as TB and cancer.

Previously Paul worked within the BioPharma industry (GSK, Astex Therapeutics) for 23 years, gaining experience across a range of therapeutic areas. He played a significant part in seven compounds entering pre-clinical development, two of which are now in Phase II clinical trials. Paul obtained his BSc and PhD in Chemistry from the University of Birmingham. Paul has published around 50 papers and he is an inventor on over 35 patent applications.

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University of Dundee: Dundee, Dundee, GB

2006-03-16 to present | Head of Drug Discovery Unit (Drug Discovery Unit)

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Paul G Wyatt

https://orcid.org/0000-0002-0397-245X

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Biography

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Employment (4)

University of Dundee: Dundee, Dundee, GB

Astex Pharmaceuticals European office: Cambridge, Cambridgeshire, GB

Glaxo, GlaxoWellcome, GlaxoSmithKline: Greenford, Stevenage, GB

Beecham, SmithKlineBeecham: Epsom, GB

Education and qualifications (2)

University of Birmingham: Birmingham, GB

University of Birmingham: Birmigham, GB

Works (50 of 51)

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

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

Exploring the Trypanosoma brucei Hsp83 Potential as a Target for Structure Guided Drug Design

Fragment-based hit identification: Thinking in 3D

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

Structure-activity relationship studies of pyrrolone antimalarial agents

Chemical proteomic analysis reveals the drugability of the kinome of trypanosoma brucei

Design, synthesis and biological evaluation of Trypanosoma brucei Trypanothione Synthetase inhibitors

Discovery of a novel class of orally active trypanocidal N-Myristoyltransferase inhibitors

Quinol derivatives as potential trypanocidal agents

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

Design, Synthesis and Biological Evaluation of Novel Inhibitors of Trypanosoma brucei Pteridine Reductase1

Dihydroquinazolines as a novel class of Trypanosoma brucei trypanothione reductase inhibitors: Discovery, synthesis, and characterization of their binding mode by protein crystallography

Identification of Inhibitors of the Leishmania cdc2-Related Protein Kinase CRK3

Optimisation of the Anti-Trypanosoma brucei Activity of the Opioid Agonist U50488

Progress in neglected disease drug discovery

Target validation: Linking target and chemical properties to desired product profile

Drug discovery in academia: The third way?

N-myristoyltransferase inhibitors as new leads to treat sleeping sickness

Nuclear DBF-2-related kinases are essential regulators of cytokinesis in bloodstream stage Trypanosoma brucei

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

Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity

Investigation of trypanothione reductase as a drug target in Trypanosoma brucei

One scaffold, three binding modes: Novel and selective pteridine reductase 1 inhibitors derived from fragment hits discovered by virtual screening

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

The emerging academic drug-discovery sector

Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H- pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design

Lessons learnt from assembling screening libraries for drug discovery for neglected diseases

Identification of inhibitors of protein kinase B using fragment-based lead discovery

Target assessment for antiparasitic drug discovery

Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B

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

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

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

A novel and efficient regiospecific preparation of arenesulfonamide derivatives of 3,5-diamino-1,2,4-triazole

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

Identification of potent and selective oxytocin antagonists. Part 2: Further investigation of benzofuran derivatives

Sialidase inhibitors related to zanamivir. Further SAR studies of 4-amino-4H-pyran-2-carboxylic acid-6-propylamides

Structure-activity relationship investigations of a potent and selective benzodiazepine oxytocin antagonist

Dihydropyrancarboxamides related to zanamivir: A new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino- 4H-pyran-6-carboxamides

A short high yielding synthesis of the potent anti-VZV carbocyclic nucleoside analogue carba-BVDU

Approaches to carbocyclic analogues of the potent neuraminidase inhibitor 4-guanidino-Neu5Ac2en. X-ray molecular structure of N-[(1S,2S,6R)-2-azido-6- benzyloxymethyl-4-formylcyclohex-3-enyl]acetamide

Benzophenone derivatives: A novel series of potent and selective inhibitors of human immunodeficiency virus type 1 reverse transcriptase

Synthesis and structure activity relationships of a series of penicillin- derived pseudosymmetric inhibitors of HIV-1 proteinase

Synthesis, oral bioavailability and in vivo activity of acetal derivatives of the selective antiherpesvirus agent 9-(3-hydroxypropoxy) guanine (BRL 44385)

A series of penicillin derived C2-symmetric inhibitors of HIV-1 proteinase: Synthesis, mode of interaction, and structure-activity relationships

Synthesis and antiviral activity of 9-alkoxypurines. 1. 9-(3-hydroxypropoxy)- and 9-[3-hydroxy-2-(hydroxymethyl)propoxy]purines

Synthesis of 9-hydroxypurines: Intermediates to novel antiviral acyclonucleosides

Analogues of the antiviral acyclonucleoside 9-(4-hydroxy-3-hydroxymethylbutyl)guanine. Part 1. Substitutions on C-2′ of the acyclic N-9 substituent

Synthesis of 9-(3-hydroxypropoxy)guanine, a novel antiviral acyclonucleoside

Peer review (1 review for 1 publication/grant)