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Molecular basis of USP7 inhibition by selective small-molecule inhibitors.
Turnbull AP, Ioannidis S, Krajewski WW, Pinto-Fernandez A, Heride C, Martin ACL, Tonkin LM, Townsend EC, Buker SM, Lancia DR, Caravella JA, Toms AV, Charlton TM, Lahdenranta J, Wilker E, Follows BC, Evans NJ, Stead L, Alli C, Zarayskiy VV, Talbot AC, Buckmelter AJ, Wang M, McKinnon CL, Saab F, McGouran JF, Century H, Gersch M, Pittman MS, Marshall CG, Raynham TM, Simcox M, Stewart LMD, McLoughlin SB, Escobedo JA, Bair KW, Dinsmore CJ, Hammonds TR, Kim S, Urbé S, Clague MJ, Kessler BM, Komander D. Turnbull AP, et al. Among authors: toms av. Nature. 2017 Oct 26;550(7677):481-486. doi: 10.1038/nature24451. Epub 2017 Oct 18. Nature. 2017. PMID: 29045389 Free PMC article.
Discovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors.
Lin J, Lu W, Caravella JA, Campbell AM, Diebold RB, Ericsson A, Fritzen E, Gustafson GR, Lancia DR Jr, Shelekhin T, Wang Z, Castro J, Clarke A, Gotur D, Josephine HR, Katz M, Diep H, Kershaw M, Yao L, Kauffman G, Hubbs SE, Luke GP, Toms AV, Wang L, Bair KW, Barr KJ, Dinsmore C, Walker D, Ashwell S. Lin J, et al. Among authors: toms av. J Med Chem. 2019 Jul 25;62(14):6575-6596. doi: 10.1021/acs.jmedchem.9b00362. Epub 2019 Jul 8. J Med Chem. 2019. PMID: 31199148
Structure-Based Design and Identification of FT-2102 (Olutasidenib), a Potent Mutant-Selective IDH1 Inhibitor.
Caravella JA, Lin J, Diebold RB, Campbell AM, Ericsson A, Gustafson G, Wang Z, Castro J, Clarke A, Gotur D, Josephine HR, Katz M, Kershaw M, Yao L, Toms AV, Barr KJ, Dinsmore CJ, Walker D, Ashwell S, Lu W. Caravella JA, et al. Among authors: toms av. J Med Chem. 2020 Feb 27;63(4):1612-1623. doi: 10.1021/acs.jmedchem.9b01423. Epub 2020 Feb 12. J Med Chem. 2020. PMID: 31971798
Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN).
Martin MW, Lancia DR Jr, Li H, Schiller SER, Toms AV, Wang Z, Bair KW, Castro J, Fessler S, Gotur D, Hubbs SE, Kauffman GS, Kershaw M, Luke GP, McKinnon C, Yao L, Lu W, Millan DS. Martin MW, et al. Among authors: toms av. Bioorg Med Chem Lett. 2019 Apr 15;29(8):1001-1006. doi: 10.1016/j.bmcl.2019.02.012. Epub 2019 Feb 11. Bioorg Med Chem Lett. 2019. PMID: 30803804
Potent and selective TYK2-JH1 inhibitors highly efficacious in rodent model of psoriasis.
Leit S, Greenwood JR, Mondal S, Carriero S, Dahlgren M, Harriman GC, Kennedy-Smith JJ, Kapeller R, Lawson JP, Romero DL, Toms AV, Shelley M, Wester RT, Westlin W, McElwee JJ, Miao W, Edmondson SD, Masse CE. Leit S, et al. Among authors: toms av. Bioorg Med Chem Lett. 2022 Oct 1;73:128891. doi: 10.1016/j.bmcl.2022.128891. Epub 2022 Jul 13. Bioorg Med Chem Lett. 2022. PMID: 35842205
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.
Huang WS, Liu S, Zou D, Thomas M, Wang Y, Zhou T, Romero J, Kohlmann A, Li F, Qi J, Cai L, Dwight TA, Xu Y, Xu R, Dodd R, Toms A, Parillon L, Lu X, Anjum R, Zhang S, Wang F, Keats J, Wardwell SD, Ning Y, Xu Q, Moran LE, Mohemmad QK, Jang HG, Clackson T, Narasimhan NI, Rivera VM, Zhu X, Dalgarno D, Shakespeare WC. Huang WS, et al. J Med Chem. 2016 May 26;59(10):4948-64. doi: 10.1021/acs.jmedchem.6b00306. Epub 2016 May 12. J Med Chem. 2016. PMID: 27144831
Crystal Structure of the FERM-SH2 Module of Human Jak2.
McNally R, Toms AV, Eck MJ. McNally R, et al. Among authors: toms av. PLoS One. 2016 May 26;11(5):e0156218. doi: 10.1371/journal.pone.0156218. eCollection 2016. PLoS One. 2016. PMID: 27227461 Free PMC article.
21 results