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.

2019

WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop.

Agajanian MJ, Walker MP, Axtman AD, Ruela-de-Sousa RR, Serafin DS, Rabinowitz AD, Graham DM, Ryan MB, Tamir T, Nakamichi Y, Gammons MV, Bennett JM, Couñago RM, Drewry DH, Elkins JM, Gileadi C, Gileadi O, Godoi PH, Kapadia N, Müller S, Santiago AS, Sorrell FJ, Wells CI, Fedorov O, Willson TM, Zuercher WJ, Major MB

Cell Rep. 2019-1-2 . 26(1):79-93.e8 .doi: 10.1016/j.celrep.2018.12.023

PMID: 30605688

2018

1,2,6-Thiadiazinones as Novel Narrow Spectrum Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CaMKK2) Inhibitors.

Asquith CRM, Godoi PH, Couñago RM, Laitinen T, Scott JW, Langendorf CG, Oakhill JS, Drewry DH, Zuercher WJ, Koutentis PA, Willson TM, Kalogirou AS

Molecules. 2018-5-19 . 23(5): .doi: 10.3390/molecules23051221

PMID: 29783765

Application of Integrated Drug Screening/Kinome Analysis to Identify Inhibitors of Gemcitabine-Resistant Pancreatic Cancer Cell Growth.

Krulikas LJ, McDonald IM, Lee B, Okumu DO, East MP, Gilbert TSK, Herring LE, Golitz BT, Wells CI, Axtman AD, Zuercher WJ, Willson TM, Kireev D, Yeh JJ, Johnson GL, Baines AT, Graves LM

SLAS Discov. 2018-5-1 . 2472555218773045 .doi: 10.1177/2472555218773045

PMID: 29742358

Donated chemical probes for open science.

Müller S, Ackloo S, Arrowsmith CH, Bauser M, Baryza JL, Blagg J, Böttcher J, Bountra C, Brown PJ, Bunnage ME, Carter AJ, Damerell D, Dötsch V, Drewry DH, Edwards AM, Edwards J, Elkins JM, Fischer C, Frye SV, Gollner A, Grimshaw CE, IJzerman A, Hanke T, Hartung IV, Hitchcock S, Howe T, Hughes TV, Laufer S, Li VM, Liras S, Marsden BD, Matsui H, Mathias J, O'Hagan RC, Owen DR, Pande V, Rauh D, Rosenberg SH, Roth BL, Schneider NS, Scholten C, Singh Saikatendu K, Simeonov A, Takizawa M, Tse C, Thompson PR, Treiber DK, Viana AY, Wells CI, Willson TM, Zuercher WJ, Knapp S, Mueller-Fahrnow A

Elife. 2018-4-20 . 7: .doi: 10.7554/eLife.34311

PMID: 29676732

Circadian clock component REV-ERBα controls homeostatic regulation of pulmonary inflammation.

Pariollaud M, Gibbs J, Hopwood T, Brown S, Begley N, Vonslow R, Poolman T, Guo B, Saer B, Jones DH, Tellam JP, Bresciani S, Tomkinson NC, Wojno-Picon J, Cooper AW, Daniels DA, Trump RP, Grant D, Zuercher W, Willson TM, MacDonald AS, Bolognese B, Podolin PL, Sanchez Y, Loudon AS, Ray DW

J. Clin. Invest.. 2018-3-13 . .doi: 10.1172/JCI93910

PMID: 29533925

2017

Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement.

Vasta JD, Corona CR, Wilkinson J, Zimprich CA, Hartnett JR, Ingold MR, Zimmerman K, Machleidt T, Kirkland TA, Huwiler KG, Ohana RF, Slater M, Otto P, Cong M, Wells CI, Berger BT, Hanke T, Glas C, Ding K, Drewry DH, Huber KVM, Willson TM, Knapp S, Müller S, Meisenheimer PL, Fan F, Wood KV, Robers MB

Cell Chem Biol. 2017-11-13 . .doi: 10.1016/j.chembiol.2017.10.010

PMID: 29174542

Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase.

Asquith CRM, Laitinen T, Bennett JM, Godoi PH, East MP, Tizzard GJ, Graves LM, Johnson GL, Dornsife RE, Wells CI, Elkins JM, Willson TM, Zuercher W

ChemMedChem. 2017-10-26 . .doi: 10.1002/cmdc.201700663

PMID: 29072804

Progress towards a public chemogenomic set for protein kinases and a call for contributions.

Drewry DH, Wells CI, Andrews DM, Angell R, Al-Ali H, Axtman AD, Capuzzi SJ, Elkins JM, Ettmayer P, Frederiksen M, Gileadi O, Gray N, Hooper A, Knapp S, Laufer S, Luecking U, Michaelides M, Müller S, Muratov E, Denny RA, Saikatendu KS, Treiber DK, Zuercher WJ, Willson TM

PLoS ONE. 2017-8-3 . 12(8):e0181585 .doi: 10.1371/journal.pone.0181585

PMID: 28767711

2015

Comprehensive characterization of the Published Kinase Inhibitor Set.

Elkins JM, Fedele V, Szklarz M, Abdul Azeez KR, Salah E, Mikolajczyk J, Romanov S, Sepetov N, Huang XP, Roth BL, Al Haj Zen A, Fourches D, Muratov E, Tropsha A, Morris J, Teicher BA, Kunkel M, Polley E, Lackey KE, Atkinson FL, Overington JP, Bamborough P, Müller S, Price DJ, Willson TM, Drewry DH, Knapp S, Zuercher WJ

Nat. Biotechnol.. 2015-10-26 . .doi: 10.1038/nbt.3374

PMID: 26501955

The promise and peril of chemical probes.

Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ

Nat. Chem. Biol.. 2015-7-21 . 11(8):536-41 .doi: 10.1038/nchembio.1867

PMID: 26196764