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Page 1
Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer.
Sharma S, Chung CY, Uryu S, Petrovic J, Cao J, Rickard A, Nady N, Greasley S, Johnson E, Brodsky O, Khan S, Wang H, Wang Z, Zhang Y, Tsaparikos K, Chen L, Mazurek A, Lapek J, Kung PP, Sutton S, Richardson PF, Greenwald EC, Yamazaki S, Jones R, Maegley KA, Bingham P, Lam H, Stupple AE, Kamal A, Chueh A, Cuzzupe A, Morrow BJ, Ren B, Carrasco-Pozo C, Tan CW, Bhuva DD, Allan E, Surgenor E, Vaillant F, Pehlivanoglu H, Falk H, Whittle JR, Newman J, Cursons J, Doherty JP, White KL, MacPherson L, Devlin M, Dennis ML, Hattarki MK, De Silva M, Camerino MA, Butler MS, Dolezal O, Pilling P, Foitzik R, Stupple PA, Lagiakos HR, Walker SR, Hediyeh-Zadeh S, Nuttall S, Spall SK, Charman SA, Connor T, Peat TS, Avery VM, Bozikis YE, Yang Y, Zhang M, Monahan BJ, Voss AK, Thomas T, Street IP, Dawson SJ, Dawson MA, Lindeman GJ, Davis MJ, Visvader JE, Paul TA. Sharma S, et al. Among authors: pilling p. Cell Chem Biol. 2023 Oct 19;30(10):1191-1210.e20. doi: 10.1016/j.chembiol.2023.07.005. Epub 2023 Aug 8. Cell Chem Biol. 2023. PMID: 37557181 Free article.
Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth.
Baell JB, Leaver DJ, Hermans SJ, Kelly GL, Brennan MS, Downer NL, Nguyen N, Wichmann J, McRae HM, Yang Y, Cleary B, Lagiakos HR, Mieruszynski S, Pacini G, Vanyai HK, Bergamasco MI, May RE, Davey BK, Morgan KJ, Sealey AJ, Wang B, Zamudio N, Wilcox S, Garnham AL, Sheikh BN, Aubrey BJ, Doggett K, Chung MC, de Silva M, Bentley J, Pilling P, Hattarki M, Dolezal O, Dennis ML, Falk H, Ren B, Charman SA, White KL, Rautela J, Newbold A, Hawkins ED, Johnstone RW, Huntington ND, Peat TS, Heath JK, Strasser A, Parker MW, Smyth GK, Street IP, Monahan BJ, Voss AK, Thomas T. Baell JB, et al. Among authors: pilling p. Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub 2018 Aug 1. Nature. 2018. PMID: 30069049
Characterization of the novel broad-spectrum kinase inhibitor CTx-0294885 as an affinity reagent for mass spectrometry-based kinome profiling.
Zhang L, Holmes IP, Hochgräfe F, Walker SR, Ali NA, Humphrey ES, Wu J, de Silva M, Kersten WJ, Connor T, Falk H, Allan L, Street IP, Bentley JD, Pilling PA, Monahan BJ, Peat TS, Daly RJ. Zhang L, et al. Among authors: pilling pa. J Proteome Res. 2013 Jul 5;12(7):3104-16. doi: 10.1021/pr3008495. Epub 2013 Jun 25. J Proteome Res. 2013. PMID: 23692254
Unprecedented conformational flexibility revealed in the ligand-binding domains of the Bovicola ovis ecdysone receptor (EcR) and ultraspiracle (USP) subunits.
Ren B, Peat TS, Streltsov VA, Pollard M, Fernley R, Grusovin J, Seabrook S, Pilling P, Phan T, Lu L, Lovrecz GO, Graham LD, Hill RJ. Ren B, et al. Among authors: pilling p. Acta Crystallogr D Biol Crystallogr. 2014 Jul;70(Pt 7):1954-64. doi: 10.1107/S1399004714009626. Epub 2014 Jun 29. Acta Crystallogr D Biol Crystallogr. 2014. PMID: 25004972
Reduced abundance of the E3 ubiquitin ligase E6AP contributes to decreased expression of the INK4/ARF locus in non-small cell lung cancer.
Gamell C, Gulati T, Levav-Cohen Y, Young RJ, Do H, Pilling P, Takano E, Watkins N, Fox SB, Russell P, Ginsberg D, Monahan BJ, Wright G, Dobrovic A, Haupt S, Solomon B, Haupt Y. Gamell C, et al. Among authors: pilling p. Sci Signal. 2017 Jan 10;10(461):eaaf8223. doi: 10.1126/scisignal.aaf8223. Sci Signal. 2017. PMID: 28074012
A human monoclonal antibody against insulin-like growth factor-II blocks the growth of human hepatocellular carcinoma cell lines in vitro and in vivo.
Dransfield DT, Cohen EH, Chang Q, Sparrow LG, Bentley JD, Dolezal O, Xiao X, Peat TS, Newman J, Pilling PA, Phan T, Priebe I, Brierley GV, Kastrapeli N, Kopacz K, Martik D, Wassaf D, Rank D, Conley G, Huang Y, Adams TE, Cosgrove L. Dransfield DT, et al. Mol Cancer Ther. 2010 Jun;9(6):1809-19. doi: 10.1158/1535-7163.MCT-09-1134. Epub 2010 Jun 1. Mol Cancer Ther. 2010. PMID: 20515953
c-Abl phosphorylates E6AP and regulates its E3 ubiquitin ligase activity.
Chan AL, Grossman T, Zuckerman V, Campigli Di Giammartino D, Moshel O, Scheffner M, Monahan B, Pilling P, Jiang YH, Haupt S, Schueler-Furman O, Haupt Y. Chan AL, et al. Among authors: pilling p. Biochemistry. 2013 May 7;52(18):3119-29. doi: 10.1021/bi301710c. Epub 2013 Apr 26. Biochemistry. 2013. PMID: 23581475
The X-ray structure of a hemipteran ecdysone receptor ligand-binding domain: comparison with a lepidopteran ecdysone receptor ligand-binding domain and implications for insecticide design.
Carmichael JA, Lawrence MC, Graham LD, Pilling PA, Epa VC, Noyce L, Lovrecz G, Winkler DA, Pawlak-Skrzecz A, Eaton RE, Hannan GN, Hill RJ. Carmichael JA, et al. J Biol Chem. 2005 Jun 10;280(23):22258-69. doi: 10.1074/jbc.M500661200. Epub 2005 Apr 4. J Biol Chem. 2005. PMID: 15809296 Free article.
21 results