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Page 1
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. Among authors: mcwhirter c. Nat Commun. 2021 Jun 17;12(1):3636. doi: 10.1038/s41467-021-23463-8. Nat Commun. 2021. PMID: 34140467 Free PMC article.
Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor.
Rodrik-Outmezguine VS, Okaniwa M, Yao Z, Novotny CJ, McWhirter C, Banaji A, Won H, Wong W, Berger M, de Stanchina E, Barratt DG, Cosulich S, Klinowska T, Rosen N, Shokat KM. Rodrik-Outmezguine VS, et al. Among authors: mcwhirter c. Nature. 2016 Jun 9;534(7606):272-6. doi: 10.1038/nature17963. Epub 2016 May 18. Nature. 2016. PMID: 27279227 Free PMC article.
Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase Theta.
Stockley ML, Ferdinand A, Benedetti G, Blencowe P, Boyd SM, Calder M, Charles MD, Edwardes LV, Ekwuru T, Finch H, Galbiati A, Geo L, Grande D, Grinkevich V, Holliday ND, Krajewski WW, MacDonald E, Majithiya JB, McCarron H, McWhirter CL, Patel V, Pedder C, Rajendra E, Ranzani M, Rigoreau LJM, Robinson HMR, Schaedler T, Sirina J, Smith GCM, Swarbrick ME, Turnbull AP, Willis S, Heald RA. Stockley ML, et al. Among authors: mcwhirter cl. J Med Chem. 2022 Oct 27;65(20):13879-13891. doi: 10.1021/acs.jmedchem.2c01142. Epub 2022 Oct 6. J Med Chem. 2022. PMID: 36200480
Correction to "Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase Theta".
Stockley ML, Benedetti G, Blencowe P, Boulton SJ, Boyd SM, Calder M, Charles MD, Edwardes LV, Ekwuru T, Ferdinand A, Finch H, Galbiati A, Geo L, Grande D, Grinkevich V, Higgins GS, Holliday ND, Krajewski WW, MacDonald E, Majithiya JB, McCarron H, McWhirter CL, Patel V, Pedder C, Rajendra E, Ranzani M, Rigoreau LJM, Robinson HMR, Schaedler T, Sirina J, Smith GCM, Swarbrick ME, Turnbull AP, Willis S, Zemla A, Heald RA. Stockley ML, et al. Among authors: mcwhirter cl. J Med Chem. 2023 Feb 23. doi: 10.1021/acs.jmedchem.3c00204. Online ahead of print. J Med Chem. 2023. PMID: 36815444 No abstract available.
Cellularly active N-hydroxyurea FEN1 inhibitors block substrate entry to the active site.
Exell JC, Thompson MJ, Finger LD, Shaw SJ, Debreczeni J, Ward TA, McWhirter C, Siöberg CL, Martinez Molina D, Abbott WM, Jones CD, Nissink JW, Durant ST, Grasby JA. Exell JC, et al. Among authors: mcwhirter c. Nat Chem Biol. 2016 Oct;12(10):815-21. doi: 10.1038/nchembio.2148. Epub 2016 Aug 15. Nat Chem Biol. 2016. PMID: 27526030 Free PMC article.
Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance.
Finlay MRV, Barton P, Bickerton S, Bista M, Colclough N, Cross DAE, Evans L, Floc'h N, Gregson C, Guérot CM, Hargreaves D, Kang X, Lenz EM, Li X, Liu Y, Lorthioir O, Martin MJ, McKerrecher D, McWhirter C, O'Neill D, Orme JP, Mosallanejad A, Rahi A, Smith PD, Talbot V, Ward RA, Wrigley G, Wylot M, Xue L, Yao T, Ye Y, Zhao X. Finlay MRV, et al. Among authors: mcwhirter c. J Med Chem. 2021 Sep 23;64(18):13704-13718. doi: 10.1021/acs.jmedchem.1c01055. Epub 2021 Sep 7. J Med Chem. 2021. PMID: 34491761
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma.
Scott JS, Degorce SL, Anjum R, Culshaw J, Davies RDM, Davies NL, Dillman KS, Dowling JE, Drew L, Ferguson AD, Groombridge SD, Halsall CT, Hudson JA, Lamont S, Lindsay NA, Marden SK, Mayo MF, Pease JE, Perkins DR, Pink JH, Robb GR, Rosen A, Shen M, McWhirter C, Wu D. Scott JS, et al. Among authors: mcwhirter c. J Med Chem. 2017 Dec 28;60(24):10071-10091. doi: 10.1021/acs.jmedchem.7b01290. Epub 2017 Dec 11. J Med Chem. 2017. PMID: 29172502
36 results