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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: downer nl. Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub 2018 Aug 1. Nature. 2018. PMID: 30069049
MOZ (MYST3, KAT6A) inhibits senescence via the INK4A-ARF pathway.
Sheikh BN, Phipson B, El-Saafin F, Vanyai HK, Downer NL, Bird MJ, Kueh AJ, May RE, Smyth GK, Voss AK, Thomas T. Sheikh BN, et al. Among authors: downer nl. Oncogene. 2015 Nov 19;34(47):5807-20. doi: 10.1038/onc.2015.33. Epub 2015 Mar 16. Oncogene. 2015. PMID: 25772242
Discovery of Acylsulfonohydrazide-Derived Inhibitors of the Lysine Acetyltransferase, KAT6A, as Potent Senescence-Inducing Anti-Cancer Agents.
Priebbenow DL, Leaver DJ, Nguyen N, Cleary B, Lagiakos HR, Sanchez J, Xue L, Huang F, Sun Y, Mujumdar P, Mudududdla R, Varghese S, Teguh S, Charman SA, White KL, Shackleford DM, Katneni K, Cuellar M, Strasser JM, Dahlin JL, Walters MA, Street IP, Monahan BJ, Jarman KE, Jousset Sabroux H, Falk H, Chung MC, Hermans SJ, Downer NL, Parker MW, Voss AK, Thomas T, Baell JB. Priebbenow DL, et al. Among authors: downer nl. J Med Chem. 2020 May 14;63(9):4655-4684. doi: 10.1021/acs.jmedchem.9b02071. Epub 2020 Mar 19. J Med Chem. 2020. PMID: 32118427
Homozygous TAF8 mutation in a patient with intellectual disability results in undetectable TAF8 protein, but preserved RNA polymerase II transcription.
El-Saafin F, Curry C, Ye T, Garnier JM, Kolb-Cheynel I, Stierle M, Downer NL, Dixon MP, Negroni L, Berger I, Thomas T, Voss AK, Dobyns W, Devys D, Tora L. El-Saafin F, et al. Among authors: downer nl. Hum Mol Genet. 2018 Jun 15;27(12):2171-2186. doi: 10.1093/hmg/ddy126. Hum Mol Genet. 2018. PMID: 29648665 Free PMC article.