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Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C.
Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Boyd S, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Davies NL, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Hanson L, Harlfinger S, Howard M, Howells R, Jackson A, Kemmitt P, Lamont G, Lamont S, Lewis HJ, Liu L, Niedbala MJ, Phillips C, Polanski R, Raubo P, Robb G, Robinson DM, Ross S, Sanders MG, Tonge M, Whiteley R, Wilkinson S, Yang J, Zhang W. Kettle JG, et al. Among authors: wilkinson s. J Med Chem. 2022 May 12;65(9):6940-6952. doi: 10.1021/acs.jmedchem.2c00369. Epub 2022 Apr 26. J Med Chem. 2022. PMID: 35471939
Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors.
Degorce SL, Aagaard A, Anjum R, Cumming IA, Diène CR, Fallan C, Johnson T, Leuchowius KJ, Orton AL, Pearson S, Robb GR, Rosen A, Scarfe GB, Scott JS, Smith JM, Steward OR, Terstiege I, Tucker MJ, Turner P, Wilkinson SD, Wrigley GL, Xue Y. Degorce SL, et al. Among authors: wilkinson sd. Bioorg Med Chem. 2020 Dec 1;28(23):115815. doi: 10.1016/j.bmc.2020.115815. Epub 2020 Oct 15. Bioorg Med Chem. 2020. PMID: 33091850
Optimization of an Imidazo[1,2-a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy.
McCoull W, Boyd S, Brown MR, Coen M, Collingwood O, Davies NL, Doherty A, Fairley G, Goldberg K, Hardaker E, He G, Hennessy EJ, Hopcroft P, Hodgson G, Jackson A, Jiang X, Karmokar A, Lainé AL, Lindsay N, Mao Y, Markandu R, McMurray L, McLean N, Mooney L, Musgrove H, Nissink JWM, Pflug A, Reddy VP, Rawlins PB, Rivers E, Schimpl M, Smith GF, Tentarelli S, Travers J, Troup RI, Walton J, Wang C, Wilkinson S, Williamson B, Winter-Holt J, Yang D, Zheng Y, Zhu Q, Smith PD. McCoull W, et al. Among authors: wilkinson s. J Med Chem. 2021 Sep 23;64(18):13524-13539. doi: 10.1021/acs.jmedchem.1c00920. Epub 2021 Sep 3. J Med Chem. 2021. PMID: 34478292
Optimization of Potent, Efficacious, Selective and Blood-Brain Barrier Penetrating Inhibitors Targeting EGFR Exon20 Insertion Mutations.
Thomson C, Braybrooke E, Colclough N, Davies NL, Floc'h N, Greenwood R, Guérot C, Hargreaves D, Johnstrom P, Khurana P, Kostomiris DH, Li S, Lister A, Lorthioir O, Martin S, McCoull W, McLean NJ, McWilliams L, Orme JP, Packer MJ, Pearson S, Swaih AM, Tentarelli S, Tucker MJ, Ward RA, Wilkinson S, Winlow P, Wood IL. Thomson C, et al. Among authors: wilkinson s. J Med Chem. 2024 Sep 28. doi: 10.1021/acs.jmedchem.4c01792. Online ahead of print. J Med Chem. 2024. PMID: 39340451
Low tristetraprolin expression activates phenotypic plasticity and primes transition to lethal prostate cancer in mice.
Morel KL, Germán B, Hamid AA, Nanda JS, Linder S, Bergman AM, van der Poel H, Hofland I, Bekers EM, Trostel SY, Burkhart DL, Wilkinson S, Ku AT, Kim M, Kim J, Ma D, Plummer JT, You S, Su XA, Zwart W, Sowalsky AG, Sweeney CJ, Ellis L. Morel KL, et al. Among authors: wilkinson s. J Clin Invest. 2024 Nov 19:e175680. doi: 10.1172/JCI175680. Online ahead of print. J Clin Invest. 2024. PMID: 39560993 Free article.
1,711 results