Tim Willson

Tim Willson

SGC UNC

Willson

Tim Willson

(919) 491-3177
1062 Genetic Medicine Buildin, 120 Mason Farms Road, CB# 7356, Chapel Hill, NC, 27599

Biography

Tim Willson is chief scientist of the SGC-UNC, an open-discovery network for protein kinases based at the UNC Eshelman School of Pharmacy. He has more than 25 years of experience in pharmaceutical research with a track record in discovery of first-in-class clinical candidates. Throughout his career, Willson has been an advocate for research on pioneer drug targets. He led the Glaxo program on orphan nuclear receptors that uncovered their role in regulation of human metabolism and was co-discoverer of obeticholic acid, a breakthrough medicine for liver diseases targeting FXR. Willson has been a long time supporter of precompetitive chemistry in early drug discovery and was a scientific founder of the SGC Epigenetic Chemical Probes project. He is widely recognized for scientific leadership in chemical biology and was named one of the world’s 400 most influential biomedical researchers. Outside of science, Willson enjoys the challenge of long course triathlons and has completed six Ironman 70.3 distance races.

Research Areas

Willson has been a long-time supporter of precompetitive chemistry as a mechanism to bring innovation to early drug discovery. His team has made potent and selective chemical probes for orphan nuclear receptors widely available in the scientific community. He was a scientific founder of the SGC Epigenetic Chemical Probes project that led to the release into the public domain of more than 30 chemical probes that specifically inhibit enzyme modifiers and protein readers of the histone tails.

2021

The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification.

Wells CI, Al-Ali H, Andrews DM, Asquith CRM, Axtman AD, Dikic I, Ebner D, Ettmayer P, Fischer C, Frederiksen M, Futrell RE, Gray NS, Hatch SB, Knapp S, Lücking U, Michaelides M, Mills CE, Müller S, Owen D, Picado A, Saikatendu KS, Schröder M, Stolz A, Tellechea M, Turunen BJ, Vilar S, Wang J, Zuercher WJ, Willson TM, Drewry DH

Int J Mol Sci. 2021-1-8 . 22(2): .doi: 10.3390/ijms22020566

PMID: 33429995

2020

A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation.

Picado A, Chaikuad A, Wells CI, Shrestha S, Zuercher WJ, Pickett JE, Kwarcinski FE, Sinha P, de Silva CS, Zutshi R, Liu S, Kannan N, Knapp S, Drewry DH, Willson TM

J Med Chem. 2020-11-20 . .doi: 10.1021/acs.jmedchem.0c01174

PMID: 33215924

Quantifying CDK inhibitor selectivity in live cells.

Wells CI, Vasta JD, Corona CR, Wilkinson J, Zimprich CA, Ingold MR, Pickett JE, Drewry DH, Pugh KM, Schwinn MK, Hwang BB, Zegzouti H, Huber KVM, Cong M, Meisenheimer PL, Willson TM, Robers MB

Nat Commun. 2020-6-2 . 11(1):2743 .doi: 10.1038/s41467-020-16559-0

PMID: 32488087

SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.

Wells C, Couñago RM, Limas JC, Almeida TL, Cook JG, Drewry DH, Elkins JM, Gileadi O, Kapadia NR, Lorente-Macias A, Pickett JE, Riemen A, Ruela-de-Sousa RR, Willson TM, Zhang C, Zuercher WJ, Zutshi R, Axtman AD

ACS Med Chem Lett. 2020-3-12 . 11(3):340-345 .doi: 10.1021/acsmedchemlett.9b00399

PMID: 32184967

In Depth Analysis of Kinase Cross Screening Data to Identify CAMKK2 Inhibitory Scaffolds.

O'Byrne SN, Scott JW, Pilotte JR, Santiago ADS, Langendorf CG, Oakhill JS, Eduful BJ, Couñago RM, Wells CI, Zuercher WJ, Willson TM, Drewry DH

Molecules. 2020-1-13 . 25(2): .doi: 10.3390/molecules25020325

PMID: 31941153

2019

Towards the Development of an In vivo Chemical Probe for Cyclin G Associated Kinase (GAK).

Asquith CRM, Bennett JM, Su L, Laitinen T, Elkins JM, Pickett JE, Wells CI, Li Z, Willson TM, Zuercher WJ

Molecules. 2019-11-6 . 24(22): .doi: 10.3390/molecules24224016

PMID: 31698822

Gram-scale synthesis of FICZ, a photoreactive endogenous ligand of the aryl hydrocarbon receptor.

Zhang C, Creech KL, Zuercher WJ, Willson TM

Sci Rep. 2019-7-10 . 9(1):9982 .doi: 10.1038/s41598-019-46374-7

PMID: 31292477

A Perspective on Extreme Open Science: Companies Sharing Compounds without Restriction.

Drewry DH, Wells CI, Zuercher WJ, Willson TM

SLAS Discov. 2019-4-29 . 2472555219838210 .doi: 10.1177/2472555219838210

PMID: 31034310

SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK).

Asquith CRM, Berger BT, Wan J, Bennett JM, Capuzzi SJ, Crona DJ, Drewry D, East MP, Elkins JM, Fedorov O, Godoi PH, Hunter DM, Knapp S, Müller S, Torrice CD, Wells CI, Earp HS, Willson T, Zuercher W

J. Med. Chem.. 2019-2-15 . .doi: 10.1021/acs.jmedchem.8b01213

PMID: 30768268