Tim Willson

Research Professor (UNC) - Chief Scientist (SGC)

University of North Carolina at Chapel Hill
(919) 491-3177

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.

Seeding collaborations to advance kinase science with the GSK Published Kinase Inhibitor Set (PKIS)
Drewry DH, Willson TM, Zuercher WJ.
Curr Top Med Chem. 2014 14(3):340-2. doi:
PMID: 24283969

A public-private partnership to unlock the untargeted kinome.
Knapp S, Arruda P, Blagg J, Burley S, Drewry DH, Edwards A, Fabbro D, Gillespie P, Gray NS, Kuster B, Lackey KE, Mazzafera P, Tomkinson NC, Willson TM, Workman P, Zuercher WJ
Nat. Chem. Biol.. 2012 9(1):3-6. doi: 10.1038/nchembio.1113
PMID: 23238671

Too many roads not taken.
Edwards AM, Isserlin R, Bader GD, Frye SV, Willson TM, Yu FH
Nature. 2011 470(7333):163-5. doi: 10.1038/470163a
PMID: 21307913

Open access chemical and clinical probes to support drug discovery.
Edwards AM, Bountra C, Kerr DJ, Willson TM
Nat. Chem. Biol.. 2009 5(7):436-40. doi: 10.1038/nchembio0709-436
PMID: 19536100

6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.
Pellicciari R, Fiorucci S, Camaioni E, Clerici C, Costantino G, Maloney PR, Morelli A, Parks DJ, Willson TM.
J Med Chem.. 2002 45(17):3569-72. doi:
PMID: 12166927

A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport.
Oliver WR Jr, Shenk JL, Snaith MR, Russell CS, Plunket KD, Bodkin NL, Lewis MC, Winegar DA, Sznaidman ML, Lambert MH, Xu HE, Sternbach DD, Kliewer SA, Hansen BC, Willson TM.
Proc Natl Acad Sci U S A. . 2001 98(9):5306-11.. doi:
PMID: 11309497

Identification of a chemical tool for the orphan nuclear receptor FXR
Maloney PR, Parks DJ, Haffner CD, Fivush AM, Chandra G, Plunket KD, Creech KL, Moore LB, Wilson JG, Lewis MC, Jones SA, Willson TM.
J Med Chem.. 2000 43(16):2971-4. doi:
PMID: 10956205

Orphan nuclear receptors: shifting endocrinology into reverse.
Kliewer SA, Lehmann JM, Willson TM.
Science. 1999 284(5415):757-60. doi:
PMID: 10221899

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