Tim Willson

Tim Willson

SGC UNC

Willson

Tim Willson

tim.willson@unc.edu
(919) 491-3177
1062 Genetic Medicine Buildin, 120 Mason Farms Road, CB# 7356, Chapel Hill, NC, 27599

Affiliations

UNC Eshelman School of Pharmacy

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.

  • All Publications

2024

Identification of Dihydropyrazolo[1,5-a]pyrazin-4(5H)-ones as Cyclic Products of β-Amidomethyl Vinyl Sulfone Alphavirus Cysteine Protease Inhibitors.

Ghoshal A, Magalhães ÁF, Asressu KH, Hossain MA, Todd MH, Willson TM

Pharmaceuticals (Basel). 2024-6-26 . 17(7): .doi: 10.3390/ph17070836

PMID: 39065687

STOPLIGHT: A Hit Scoring Calculator.

Wellnitz J, Martin HJ, Anwar Hossain M, Rath M, Fox C, Popov KI, Willson TM, Muratov EN, Tropsha A

J Chem Inf Model. 2024-5-20 . .doi: 10.1021/acs.jcim.4c00412

PMID: 38768560

Discovery and optimization of narrow spectrum inhibitors of Tousled like kinase 2 (TLK2) using quantitative structure activity relationships.

Asquith CRM, East MP, Laitinen T, Alamillo-Ferrer C, Hartikainen E, Wells CI, Axtman AD, Drewry DH, Tizzard GJ, Poso A, Willson TM, Johnson GL

Eur J Med Chem. 2024-4-2 . 271:116357 .doi: 10.1016/j.ejmech.2024.116357

PMID: 38636130

Synthesis of 5-Benzylamino and 5-Alkylamino-Substituted Pyrimido[4,5-c]quinoline Derivatives as CSNK2A Inhibitors with Antiviral Activity.

Asressu KH, Smith JL, Dickmander RJ, Moorman NJ, Wellnitz J, Popov KI, Axtman AD, Willson TM

Pharmaceuticals (Basel). 2024-2-27 . 17(3): .doi: 10.3390/ph17030306

PMID: 38543092

Identification of 4-(6-((2-methoxyphenyl)amino)pyrazin-2-yl)benzoic acids as CSNK2A inhibitors with antiviral activity and improved selectivity over PIM3.

Galal KA, Krämer A, Strickland BG, Smith JL, Dickmander RJ, Moorman NJ, Willson TM

Bioorg Med Chem Lett. 2024-1-8 . 99:129617 .doi: 10.1016/j.bmcl.2024.129617

PMID: 38199328

2023

Optimization of 3-Cyano-7-cyclopropylamino-pyrazolo[1,5-a]pyrimidines toward the Development of an In Vivo Chemical Probe for CSNK2A.

Yang X, Ong HW, Dickmander RJ, Smith JL, Brown JW, Tao W, Chang E, Moorman NJ, Axtman AD, Willson TM

ACS Omega. 2023-10-24 . 8(42):39546-39561 .doi: 10.1021/acsomega.3c05377

PMID: 37901516

Fused Tetrahydroquinolines Are Interfering with Your Assay.

Bashore FM, Annor-Gyamfi J, Du Y, Katis V, Nwogbo F, Flax RG, Frye SV, Pearce KH, Fu H, Willson TM, Drewry DH, Axtman AD

J Med Chem. 2023-10-24 . .doi: 10.1021/acs.jmedchem.3c01277

PMID: 37874947

Dual Inhibition of Mycobacterium tuberculosis and the Host TGFBR1 by an Anilinoquinazoline.

Nandakumar M, Ollodart A, Fleck N, Kapadia NR, Frando A, Boradia V, Smith JL, Chen J, Zuercher WJ, Willson TM, Grundner C

J Med Chem. 2023-10-23 . .doi: 10.1021/acs.jmedchem.3c01273

PMID: 37871287

Investigation of the Host Kinome Response to Coronavirus Infection Reveals PI3K/mTOR Inhibitors as Betacoronavirus Antivirals.

Fritch EJ, Mordant AL, Gilbert TSK, Wells CI, Yang X, Barker NK, Madden EA, Dinnon KH, Hou YJ, Tse LV, Castillo IN, Sims AC, Moorman NJ, Lakshmanane P, Willson TM, Herring LE, Graves LM, Baric RS

J Proteome Res. 2023-8-27 . .doi: 10.1021/acs.jproteome.3c00182

PMID: 37634194

Target 2035 - an update on private sector contributions.

Ackloo S, Antolin AA, Bartolome JM, Beck H, Bullock A, Betz UAK, Böttcher J, Brown PJ, Chaturvedi M, Crisp A, Daniels D, Dreher J, Edfeldt K, Edwards AM, Egner U, Elkins J, Fischer C, Glendorf T, Goldberg S, Hartung IV, Hillisch A, Homan E, Knapp S, Köster M, Krämer O, Llaveria J, Lessel U, Lindemann S, Linderoth L, Matsui H, Michel M, Montel F, Mueller-Fahrnow A, Müller S, Owen DR, Saikatendu KS, Santhakumar V, Sanderson W, Scholten C, Schapira M, Sharma S, Shireman B, Sundström M, Todd MH, Tredup C, Venable J, Willson TM, Arrowsmith CH

RSC Med Chem. 2023-6-22 . 14(6):1002-1011 .doi: 10.1039/d2md00441k

PMID: 37360399