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22 results

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Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase.
Hollick JJ, Rigoreau LJ, Cano-Soumillac C, Cockcroft X, Curtin NJ, Frigerio M, Golding BT, Guiard S, Hardcastle IR, Hickson I, Hummersone MG, Menear KA, Martin NM, Matthews I, Newell DR, Ord R, Richardson CJ, Smith GC, Griffin RJ. Hollick JJ, et al. Among authors: rigoreau lj. J Med Chem. 2007 Apr 19;50(8):1958-72. doi: 10.1021/jm061121y. Epub 2007 Mar 20. J Med Chem. 2007. PMID: 17371003
High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors.
Myers SM, Bawn RH, Bisset LC, Blackburn TJ, Cottyn B, Molyneux L, Wong AC, Cano C, Clegg W, Harrington RW, Leung H, Rigoreau L, Vidot S, Golding BT, Griffin RJ, Hammonds T, Newell DR, Hardcastle IR. Myers SM, et al. ACS Comb Sci. 2016 Aug 8;18(8):444-55. doi: 10.1021/acscombsci.5b00155. Epub 2016 Jul 20. ACS Comb Sci. 2016. PMID: 27400250 Free article.
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4.
Myers SM, Miller DC, Molyneux L, Arasta M, Bawn RH, Blackburn TJ, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hammonds T, Hardcastle IR, Harnor SJ, Heptinstall AB, Lochhead PA, Martin MP, Martin NC, Newell DR, Owen PJ, Pang LC, Reuillon T, Rigoreau LJM, Thomas HD, Tucker JA, Wang LZ, Wong AC, Noble MEM, Wedge SR, Cano C. Myers SM, et al. Among authors: rigoreau ljm. Eur J Med Chem. 2019 Sep 15;178:530-543. doi: 10.1016/j.ejmech.2019.05.057. Epub 2019 May 25. Eur J Med Chem. 2019. PMID: 31212132
Polθ inhibitors elicit BRCA-gene synthetic lethality and target PARP inhibitor resistance.
Zatreanu D, Robinson HMR, Alkhatib O, Boursier M, Finch H, Geo L, Grande D, Grinkevich V, Heald RA, Langdon S, Majithiya J, McWhirter C, Martin NMB, Moore S, Neves J, Rajendra E, Ranzani M, Schaedler T, Stockley M, Wiggins K, Brough R, Sridhar S, Gulati A, Shao N, Badder LM, Novo D, Knight EG, Marlow R, Haider S, Callen E, Hewitt G, Schimmel J, Prevo R, Alli C, Ferdinand A, Bell C, Blencowe P, Bot C, Calder M, Charles M, Curry J, Ekwuru T, Ewings K, Krajewski W, MacDonald E, McCarron H, Pang L, Pedder C, Rigoreau L, Swarbrick M, Wheatley E, Willis S, Wong AC, Nussenzweig A, Tijsterman M, Tutt A, Boulton SJ, Higgins GS, Pettitt SJ, Smith GCM, Lord CJ. Zatreanu D, et al. Nat Commun. 2021 Jun 17;12(1):3636. doi: 10.1038/s41467-021-23463-8. Nat Commun. 2021. PMID: 34140467 Free PMC article.
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.
Miller DC, Reuillon T, Molyneux L, Blackburn T, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hardcastle I, Harnor SJ, Heptinstall A, Lochhead P, Martin MP, Martin NC, Myers S, Newell DR, Noble RA, Phillips N, Rigoreau L, Thomas H, Tucker JA, Wang LZ, Waring MJ, Wong AC, Wedge SR, Noble MEM, Cano C. Miller DC, et al. J Med Chem. 2022 May 12;65(9):6513-6540. doi: 10.1021/acs.jmedchem.1c01756. Epub 2022 Apr 25. J Med Chem. 2022. PMID: 35468293 Free PMC article.
22 results