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Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.
Johannes JW, Balazs A, Barratt D, Bista M, Chuba MD, Cosulich S, Critchlow SE, Degorce SL, Di Fruscia P, Edmondson SD, Embrey K, Fawell S, Ghosh A, Gill SJ, Gunnarsson A, Hande SM, Heightman TD, Hemsley P, Illuzzi G, Lane J, Larner C, Leo E, Liu L, Madin A, Martin S, 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. J Med Chem. 2021 Oct 14;64(19):14498-14512. doi: 10.1021/acs.jmedchem.1c01012. Epub 2021 Sep 27. J Med Chem. 2021. PMID: 34570508
Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia.
Tron AE, Belmonte MA, Adam A, Aquila BM, Boise LH, Chiarparin E, Cidado J, Embrey KJ, Gangl E, Gibbons FD, Gregory GP, Hargreaves D, Hendricks JA, Johannes JW, Johnstone RW, Kazmirski SL, Kettle JG, Lamb ML, Matulis SM, Nooka AK, Packer MJ, Peng B, Rawlins PB, Robbins DW, Schuller AG, Su N, Yang W, Ye Q, Zheng X, Secrist JP, Clark EA, Wilson DM, Fawell SE, Hird AW. Tron AE, et al. Among authors: embrey kj. Nat Commun. 2018 Dec 17;9(1):5341. doi: 10.1038/s41467-018-07551-w. Nat Commun. 2018. PMID: 30559424 Free PMC article.
MTH1 Substrate Recognition--An Example of Specific Promiscuity.
Nissink JW, Bista M, Breed J, Carter N, Embrey K, Read J, Winter-Holt JJ. Nissink JW, et al. PLoS One. 2016 Mar 21;11(3):e0151154. doi: 10.1371/journal.pone.0151154. eCollection 2016. PLoS One. 2016. PMID: 26999531 Free PMC article.
KRAS-specific inhibition using a DARPin binding to a site in the allosteric lobe.
Bery N, Legg S, Debreczeni J, Breed J, Embrey K, Stubbs C, Kolasinska-Zwierz P, Barrett N, Marwood R, Watson J, Tart J, Overman R, Miller A, Phillips C, Minter R, Rabbitts TH. Bery N, et al. Nat Commun. 2019 Jun 13;10(1):2607. doi: 10.1038/s41467-019-10419-2. Nat Commun. 2019. PMID: 31197133 Free PMC article.
Structure guided lead generation for M. tuberculosis thymidylate kinase (Mtb TMK): discovery of 3-cyanopyridone and 1,6-naphthyridin-2-one as potent inhibitors.
Naik M, Raichurkar A, Bandodkar BS, Varun BV, Bhat S, Kalkhambkar R, Murugan K, Menon R, Bhat J, Paul B, Iyer H, Hussein S, Tucker JA, Vogtherr M, Embrey KJ, McMiken H, Prasad S, Gill A, Ugarkar BG, Venkatraman J, Read J, Panda M. Naik M, et al. Among authors: embrey kj. J Med Chem. 2015 Jan 22;58(2):753-66. doi: 10.1021/jm5012947. Epub 2014 Dec 23. J Med Chem. 2015. PMID: 25486447
Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
Collie GW, Michaelides IN, Embrey K, Stubbs CJ, Börjesson U, Dale IL, Snijder A, Barlind L, Song K, Khurana P, Phillips C, Storer RI. Collie GW, et al. ACS Med Chem Lett. 2020 Dec 8;12(1):162-167. doi: 10.1021/acsmedchemlett.0c00392. eCollection 2021 Jan 14. ACS Med Chem Lett. 2020. PMID: 33488978 Free PMC article.
Oxidation of the alarmin IL-33 regulates ST2-dependent inflammation.
Cohen ES, Scott IC, Majithiya JB, Rapley L, Kemp BP, England E, Rees DG, Overed-Sayer CL, Woods J, Bond NJ, Veyssier CS, Embrey KJ, Sims DA, Snaith MR, Vousden KA, Strain MD, Chan DT, Carmen S, Huntington CE, Flavell L, Xu J, Popovic B, Brightling CE, Vaughan TJ, Butler R, Lowe DC, Higazi DR, Corkill DJ, May RD, Sleeman MA, Mustelin T. Cohen ES, et al. Among authors: embrey kj. Nat Commun. 2015 Sep 14;6:8327. doi: 10.1038/ncomms9327. Nat Commun. 2015. PMID: 26365875 Free PMC article.
30 results