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Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor.
Johannes JW, Balazs AYS, Barratt D, Bista M, Chuba MD, Cosulich S, Critchlow SE, Degorce SL, Di Fruscia P, Edmondson SD, Embrey KJ, Fawell S, Ghosh A, Gill SJ, Gunnarsson A, Hande SM, Heightman TD, Hemsley P, Illuzzi G, Lane J, Larner CJB, Leo E, Liu L, Madin A, McWilliams L, O'Connor MJ, Orme JP, Pachl F, Packer MJ, Pei X, Pike A, Schimpl M, She H, Staniszewska AD, Talbot V, Underwood E, Varnes JG, Xue L, Yao T, Zhang K, Zhang AX, Zheng X. Johannes JW, et al. Among authors: mcwilliams l. J Med Chem. 2024 Dec 26;67(24):21717-21728. doi: 10.1021/acs.jmedchem.4c01725. Epub 2024 Dec 10. J Med Chem. 2024. PMID: 39655996
Discovery and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations.
Thomson C, Barton P, Braybrooke E, Colclough N, Dong Z, Evans L, Floc'h N, Guérot C, Hargreaves D, Khurana P, Li S, Li X, Lister A, McCoull W, McWilliams L, Orme JP, Packer MJ, Swaih AM, Ward RA, Winlow P, Ye Y. Thomson C, et al. Among authors: mcwilliams l. J Med Chem. 2024 Jun 13;67(11):8988-9027. doi: 10.1021/acs.jmedchem.4c00227. Epub 2024 May 21. J Med Chem. 2024. PMID: 38770784
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: mcwilliams l. J Med Chem. 2024 Sep 28. doi: 10.1021/acs.jmedchem.4c01792. Online ahead of print. J Med Chem. 2024. PMID: 39340451
Discovery and In Vivo Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity.
Smith JM, Barlaam B, Beattie D, Bradshaw L, Chan HM, Chiarparin E, Collingwood O, Cooke SL, Cronin A, Cumming I, Dean E, Debreczeni JÉ, Del Barco Barrantes I, Diene C, Gianni D, Guerot C, Guo X, Guven S, Hayhow TG, Hong T, Kemmitt PD, Lamont GM, Lamont S, Lynch JT, McWilliams L, Moore S, Raubo P, Robb GR, Robinson J, Scott JS, Srinivasan B, Steward O, Stubbs CJ, Syson K, Tan L, Turner O, Underwood E, Urosevic J, Vazquez-Chantada M, Whittaker AL, Wilson DM, Winter-Holt JJ. Smith JM, et al. Among authors: mcwilliams l. J Med Chem. 2024 Aug 22;67(16):13604-13638. doi: 10.1021/acs.jmedchem.4c00097. Epub 2024 Jul 30. J Med Chem. 2024. PMID: 39080842
Direct activation of KCC2 arrests benzodiazepine refractory status epilepticus and limits the subsequent neuronal injury in mice.
Jarvis R, Josephine Ng SF, Nathanson AJ, Cardarelli RA, Abiraman K, Wade F, Evans-Strong A, Fernandez-Campa MP, Deeb TZ, Smalley JL, Jamier T, Gurrell IK, McWilliams L, Kawatkar A, Conway LC, Wang Q, Burli RW, Brandon NJ, Chessell IP, Goldman AJ, Maguire JL, Moss SJ. Jarvis R, et al. Among authors: mcwilliams l. Cell Rep Med. 2023 Mar 21;4(3):100957. doi: 10.1016/j.xcrm.2023.100957. Epub 2023 Mar 7. Cell Rep Med. 2023. PMID: 36889319 Free PMC article.
Views of nutrition needs in patients with systemic sclerosis.
Samm DA, Macoustra A, Crane R, McWilliams L, Proudman S, Chapple LS. Samm DA, et al. Among authors: mcwilliams l. J Scleroderma Relat Disord. 2024 Oct;9(3):216-222. doi: 10.1177/23971983241264868. Epub 2024 Aug 8. J Scleroderma Relat Disord. 2024. PMID: 39391101
178 results