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625 results

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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: white kl. 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.
3-(Oxazolo[4,5-b]pyridin-2-yl)anilides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei, the causative agent for human African trypanosomiasis.
Ferrins L, Rahmani R, Sykes ML, Jones AJ, Avery VM, Teston E, Almohaywi B, Yin J, Smith J, Hyland C, White KL, Ryan E, Campbell M, Charman SA, Kaiser M, Baell JB. Ferrins L, et al. Among authors: white kl. Eur J Med Chem. 2013 Aug;66:450-65. doi: 10.1016/j.ejmech.2013.05.007. Epub 2013 May 16. Eur J Med Chem. 2013. PMID: 23831695
6-Arylpyrazine-2-carboxamides: A New Core for Trypanosoma brucei Inhibitors.
Rahmani R, Ban K, Jones AJ, Ferrins L, Ganame D, Sykes ML, Avery VM, White KL, Ryan E, Kaiser M, Charman SA, Baell JB. Rahmani R, et al. Among authors: white kl. J Med Chem. 2015 Sep 10;58(17):6753-65. doi: 10.1021/acs.jmedchem.5b00438. Epub 2015 Aug 30. J Med Chem. 2015. PMID: 26247439
Revisiting the SAR of the Antischistosomal Aryl Hydantoin (Ro 13-3978).
Wang C, Zhao Q, Vargas M, Jones JO, White KL, Shackleford DM, Chen G, Saunders J, Ng AC, Chiu FC, Dong Y, Charman SA, Keiser J, Vennerstrom JL. Wang C, et al. Among authors: white kl. J Med Chem. 2016 Dec 8;59(23):10705-10718. doi: 10.1021/acs.jmedchem.6b01410. Epub 2016 Nov 28. J Med Chem. 2016. PMID: 27933964 Free PMC 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: white kl. Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub 2018 Aug 1. Nature. 2018. PMID: 30069049
SAR of a new antischistosomal urea carboxylic acid.
Wu J, Wang C, Häberli C, White KL, Shackleford DM, Chen G, Dong Y, Charman SA, Keiser J, Vennerstrom JL. Wu J, et al. Among authors: white kl. Bioorg Med Chem Lett. 2018 Dec 15;28(23-24):3648-3651. doi: 10.1016/j.bmcl.2018.10.039. Epub 2018 Oct 25. Bioorg Med Chem Lett. 2018. PMID: 30389288 Free PMC article.
625 results