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

A Covalent Chemical Probe for Chikungunya nsP2 Cysteine Protease with Antialphaviral Activity and Proteome-wide Selectivity.

Ghoshal A, Tse EG, Hossain MA, Asressu KH, Merten EM, Sears JD, Howell S, Perveen S, Burdick J, Morales NL, Martinez SA, Law I, Davenport BJ, Morrison TE, Streblow ZJ, Streblow DN, Mordant AL, Webb TS, Cabrera A, Herring LE, Arrowsmith CH, Pearce KH, Moorman NJ, Heise MT, Couñago RM, Brown PJ, Willson TM

Res Sq. 2024-11-28 . .doi: 10.21203/rs.3.rs-5363451/v1

PMID: 39606462

Identification of a cell-active chikungunya virus nsP2 protease inhibitor using a covalent fragment-based screening approach.

Merten EM, Sears JD, Leisner TM, Hardy PB, Ghoshal A, Hossain MA, Asressu KH, Brown PJ, Tse EG, Stashko MA, Li K, Norris-Drouin JL, Herring LE, Mordant AL, Webb TS, Mills CA, Barker NK, Streblow ZJ, Perveen S, Arrowsmith CH, Couñago RM, Arnold JJ, Cameron CE, Streblow DN, Moorman NJ, Heise MT, Willson TM, Popov KI, Pearce KH

Proc Natl Acad Sci U S A. 2024-10-10 . 121(42):e2409166121 .doi: 10.1073/pnas.2409166121

PMID: 39388272

Strategic Fluorination to Achieve a Potent, Selective, Metabolically Stable, and Orally Bioavailable Inhibitor of CSNK2.

Ong HW, Yang X, Smith JL, Taft-Benz S, Howell S, Dickmander RJ, Havener TM, Sanders MK, Brown JW, Couñago RM, Chang E, Krämer A, Moorman NJ, Heise M, Axtman AD, Drewry DH, Willson TM

Molecules. 2024-9-14 . 29(17): .doi: 10.3390/molecules29174158

PMID: 39275006

Structure Activity of β-Amidomethyl Vinyl Sulfones as Covalent Inhibitors of Chikungunya nsP2 Cysteine Protease with Antialphavirus Activity.

Ghoshal A, Asressu KH, Hossain MA, Brown PJ, Nandakumar M, Vala A, Merten EM, Sears JD, Law I, Burdick JE, Morales NL, Perveen S, Pearce KH, Popov KI, Moorman NJ, Heise MT, Willson TM

J Med Chem. 2024-9-5 . .doi: 10.1021/acs.jmedchem.4c01346

PMID: 39235978

A data science roadmap for open science organizations engaged in early-stage drug discovery.

Edfeldt K, Edwards AM, Engkvist O, Günther J, Hartley M, Hulcoop DG, Leach AR, Marsden BD, Menge A, Misquitta L, Müller S, Owen DR, Schütt KT, Skelton N, Steffen A, Tropsha A, Vernet E, Wang Y, Wellnitz J, Willson TM, Clevert DA, Haibe-Kains B, Schiavone LH, Schapira M

Nat Commun. 2024-7-5 . 15(1):5640 .doi: 10.1038/s41467-024-49777-x

PMID: 38965235

More than an Amide Bioisostere: Discovery of 1,2,4-Triazole-containing Pyrazolo[1,5-a]pyrimidine Host CSNK2 Inhibitors for Combatting β-Coronavirus Replication.

Ong HW, Yang X, Smith JL, Dickmander RJ, Brown JW, Havener TM, Taft-Benz S, Howell S, Sanders MK, Capener JL, Couñago RM, Chang E, Krämer A, Moorman NJ, Heise M, Axtman AD, Drewry DH, Willson TM

J Med Chem. 2024-7-3 . .doi: 10.1021/acs.jmedchem.4c00962

PMID: 38959455

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