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An efficient high-throughput screening method for MYST family acetyltransferases, a new class of epigenetic drug targets.
Falk H, Connor T, Yang H, Loft KJ, Alcindor JL, Nikolakopoulos G, Surjadi RN, Bentley JD, Hattarki MK, Dolezal O, Murphy JM, Monahan BJ, Peat TS, Thomas T, Baell JB, Parisot JP, Street IP. Falk H, et al. Among authors: thomas t. J Biomol Screen. 2011 Dec;16(10):1196-205. doi: 10.1177/1087057111421631. Epub 2011 Nov 14. J Biomol Screen. 2011. PMID: 22086725
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: thomas t. Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub 2018 Aug 1. Nature. 2018. PMID: 30069049
Discovery of Benzoylsulfonohydrazides as Potent Inhibitors of the Histone Acetyltransferase KAT6A.
Leaver DJ, Cleary B, Nguyen N, Priebbenow DL, Lagiakos HR, Sanchez J, Xue L, Huang F, Sun Y, Mujumdar P, Mudududdla R, Varghese S, Teguh S, Charman SA, White KL, Katneni K, Cuellar M, Strasser JM, Dahlin JL, Walters MA, Street IP, Monahan BJ, Jarman KE, Sabroux HJ, Falk H, Chung MC, Hermans SJ, Parker MW, Thomas T, Baell JB. Leaver DJ, et al. Among authors: thomas t. J Med Chem. 2019 Aug 8;62(15):7146-7159. doi: 10.1021/acs.jmedchem.9b00665. Epub 2019 Jul 17. J Med Chem. 2019. PMID: 31256587
HBO1 is required for the maintenance of leukaemia stem cells.
MacPherson L, Anokye J, Yeung MM, Lam EYN, Chan YC, Weng CF, Yeh P, Knezevic K, Butler MS, Hoegl A, Chan KL, Burr ML, Gearing LJ, Willson T, Liu J, Choi J, Yang Y, Bilardi RA, Falk H, Nguyen N, Stupple PA, Peat TS, Zhang M, de Silva M, Carrasco-Pozo C, Avery VM, Khoo PS, Dolezal O, Dennis ML, Nuttall S, Surjadi R, Newman J, Ren B, Leaver DJ, Sun Y, Baell JB, Dovey O, Vassiliou GS, Grebien F, Dawson SJ, Street IP, Monahan BJ, Burns CJ, Choudhary C, Blewitt ME, Voss AK, Thomas T, Dawson MA. MacPherson L, et al. Among authors: thomas t. Nature. 2020 Jan;577(7789):266-270. doi: 10.1038/s41586-019-1835-6. Epub 2019 Dec 11. Nature. 2020. PMID: 31827282
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: thomas t. 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
Reference compounds for characterizing cellular injury in high-content cellular morphology assays.
Dahlin JL, Hua BK, Zucconi BE, Nelson SD Jr, Singh S, Carpenter AE, Shrimp JH, Lima-Fernandes E, Wawer MJ, Chung LPW, Agrawal A, O'Reilly M, Barsyte-Lovejoy D, Szewczyk M, Li F, Lak P, Cuellar M, Cole PA, Meier JL, Thomas T, Baell JB, Brown PJ, Walters MA, Clemons PA, Schreiber SL, Wagner BK. Dahlin JL, et al. Among authors: thomas t. Nat Commun. 2023 Mar 13;14(1):1364. doi: 10.1038/s41467-023-36829-x. Nat Commun. 2023. PMID: 36914634 Free PMC article.
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: thomas t. Oncogene. 2015 Nov 19;34(47):5807-20. doi: 10.1038/onc.2015.33. Epub 2015 Mar 16. Oncogene. 2015. PMID: 25772242
3,793 results