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.

2023

Development of Cell Permeable NanoBRET Probes for the Measurement of PLK1 Target Engagement in Live Cells.

Yang X, Smith JL, Beck MT, Wilkinson JM, Michaud A, Vasta JD, Robers MB, Willson TM

Molecules. 2023-3-25 . 28(7): .doi: 10.3390/molecules28072950

PMID: 37049713

2022

Generative and reinforcement learning approaches for the automated de novo design of bioactive compounds.

Korshunova M, Huang N, Capuzzi S, Radchenko DS, Savych O, Moroz YS, Wells CI, Willson TM, Tropsha A, Isayev O

Commun Chem. 2022-10-18 . 5(1):129 .doi: 10.1038/s42004-022-00733-0

PMID: 36697952

A New Chemotype of Chemically Tractable Nonsteroidal Estrogens Based on a Thieno[2,3-d]pyrimidine Core.

Sammeta VR, Norris JD, Artham S, Torrice CD, Byemerwa J, Joiner C, Fanning SW, McDonnell DP, Willson TM

ACS Med Chem Lett. 2022-7-14 . 13(7):1151-1158 .doi: 10.1021/acsmedchemlett.2c00180

PMID: 35859859

CACHE (Critical Assessment of Computational Hit-finding Experiments): A public-private partnership benchmarking initiative to enable the development of computational methods for hit-finding.

Ackloo S, Al-Awar R, Amaro RE, Arrowsmith CH, Azevedo H, Batey RA, Bengio Y, Betz UAK, Bologa CG, Chodera JD, Cornell WD, Dunham I, Ecker GF, Edfeldt K, Edwards AM, Gilson MK, Gordijo CR, Hessler G, Hillisch A, Hogner A, Irwin JJ, Jansen JM, Kuhn D, Leach AR, Lee AA, Lessel U, Morgan MR, Moult J, Muegge I, Oprea TI, Perry BG, Riley P, Rousseaux SAL, Saikatendu KS, Santhakumar V, Schapira M, Scholten C, Todd MH, Vedadi M, Volkamer A, Willson TM

Nat Rev Chem. 2022-7-6 . 6(4):287-295 .doi: 10.1038/s41570-022-00363-z

PMID: 35783295

Host Kinase CSNK2 is a Target for Inhibition of Pathogenic SARS-like β-Coronaviruses.

Yang X, Dickmander RJ, Bayati A, Taft-Benz SA, Smith JL, Wells CI, Madden EA, Brown JW, Lenarcic EM, Yount BL, Chang E, Axtman AD, Baric RS, Heise MT, McPherson PS, Moorman NJ, Willson TM

ACS Chem Biol. 2022-6-19 . .doi: 10.1021/acschembio.2c00378

PMID: 35723434

AD Informer Set: Chemical tools to facilitate Alzheimer's disease drug discovery.

Potjewyd FM, Annor-Gyamfi JK, Aubé J, Chu S, Conlon IL, Frankowski KJ, Guduru SKR, Hardy BP, Hopkins MD, Kinoshita C, Kireev DB, Mason ER, Moerk CT, Nwogbo F, Pearce KH, Richardson TI, Rogers DA, Soni DM, Stashko M, Wang X, Wells C, Willson TM, Frye SV, Young JE, Axtman AD

Alzheimers Dement (N Y). 2022-4-28 . 8(1):e12246 .doi: 10.1002/trc2.12246

PMID: 35475262

Use of AD Informer Set compounds to explore validity of novel targets in Alzheimer's disease pathology.

Potjewyd FM, Annor-Gyamfi JK, Aubé J, Chu S, Conlon IL, Frankowski KJ, Guduru SKR, Hardy BP, Hopkins MD, Kinoshita C, Kireev DB, Mason ER, Moerk CT, Nwogbo F, Pearce KH, Richardson TI, Rogers DA, Soni DM, Stashko M, Wang X, Wells C, Willson TM, Frye SV, Young JE, Axtman AD

Alzheimers Dement (N Y). 2022-4-19 . 8(1):e12253 .doi: 10.1002/trc2.12253

PMID: 35434254

Target 2035 - update on the quest for a probe for every protein.

Müller S, Ackloo S, Al Chawaf A, Al-Lazikani B, Antolin A, Baell JB, Beck H, Beedie S, Betz UAK, Bezerra GA, Brennan PE, Brown D, Brown PJ, Bullock AN, Carter AJ, Chaikuad A, Chaineau M, Ciulli A, Collins I, Dreher J, Drewry D, Edfeldt K, Edwards AM, Egner U, Frye SV, Fuchs SM, Hall MD, Hartung IV, Hillisch A, Hitchcock SH, Homan E, Kannan N, Kiefer JR, Knapp S, Kostic M, Kubicek S, Leach AR, Lindemann S, Marsden BD, Matsui H, Meier JL, Merk D, Michel M, Morgan MR, Mueller-Fahrnow A, Owen DR, Perry BG, Rosenberg SH, Saikatendu KS, Schapira M, Scholten C, Sharma S, Simeonov A, Sundström M, Superti-Furga G, Todd MH, Tredup C, Vedadi M, von Delft F, Willson TM, Winter GE, Workman P, Arrowsmith CH

RSC Med Chem. 2022-1-27 . 13(1):13-21 .doi: 10.1039/d1md00228g

PMID: 35211674

2021

Hinge Binder Scaffold Hopping Identifies Potent Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CAMKK2) Inhibitor Chemotypes.

Eduful BJ, O'Byrne SN, Temme L, Asquith CRM, Liang Y, Picado A, Pilotte JR, Hossain MA, Wells CI, Zuercher WJ, Catta-Preta CMC, Zonzini Ramos P, Santiago AS, Couñago RM, Langendorf CG, Nay K, Oakhill JS, Pulliam TL, Lin C, Awad D, Willson TM, Frigo DE, Scott JW, Drewry DH

J Med Chem. 2021-7-15 . .doi: 10.1021/acs.jmedchem.0c02274

PMID: 34264658

Crowdsourced mapping of unexplored target space of kinase inhibitors.

Cichońska A, Ravikumar B, Allaway RJ, Wan F, Park S, Isayev O, Li S, Mason M, Lamb A, Tanoli Z, Jeon M, Kim S, Popova M, Capuzzi S, Zeng J, Dang K, Koytiger G, Kang J, Wells CI, Willson TM, Oprea TI, Schlessinger A, Drewry DH, Stolovitzky G, Wennerberg K, Guinney J, Aittokallio T

Nat Commun. 2021-6-3 . 12(1):3307 .doi: 10.1038/s41467-021-23165-1

PMID: 34083538