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Page 1
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: lagiakos hr. 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: lagiakos hr. 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
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: lagiakos hr. 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
In Vitro and In Vivo Inhibition of the Mycobacterium tuberculosis Phosphopantetheinyl Transferase PptT by Amidinoureas.
Ottavi S, Scarry SM, Mosior J, Ling Y, Roberts J, Singh A, Zhang D, Goullieux L, Roubert C, Bacqué E, Lagiakos HR, Vendome J, Moraca F, Li K, Perkowski AJ, Ramesh R, Bowler MM, Tracy W, Feher VA, Sacchettini JC, Gold BS, Nathan CF, Aubé J. Ottavi S, et al. Among authors: lagiakos hr. J Med Chem. 2022 Feb 10;65(3):1996-2022. doi: 10.1021/acs.jmedchem.1c01565. Epub 2022 Jan 19. J Med Chem. 2022. PMID: 35044775 Free PMC article.
Empowering Voices: Inspiring Women in Medicinal Chemistry.
Blanco MJ, Bronson JJ, DiMauro EF, Dzierba C, Eggen M, Garner AL, Georg G, Giarolla J, Goodwin NC, Grenier-Davies MC, Haskell-Luevano C, Holzgrabe U, Huang R, Lagiakos HR, Leftheris K, Martin Y, Matos MJ, May-Dracka TL, Müller CE, Newman AH, Parmee E, Petter JC, Tamayo NA, Wexler RR, Bolognesi ML, Ripka A, Young W. Blanco MJ, et al. Among authors: lagiakos hr. ACS Med Chem Lett. 2024 Mar 8;15(4):424-431. doi: 10.1021/acsmedchemlett.4c00097. eCollection 2024 Apr 11. ACS Med Chem Lett. 2024. PMID: 38628790
Empowering Voices: Inspiring Women in Medicinal Chemistry.
Blanco MJ, Bronson JJ, DiMauro EF, Dzierba C, Eggen M, Garner AL, Georg G, Giarolla J, Goodwin NC, Grenier-Davies MC, Haskell-Luevano C, Holzgrabe U, Huang R, Lagiakos HR, Leftheris K, Martin Y, Matos MJ, May-Dracka TL, Müller CE, Newman AH, Parmee E, Petter JC, Tamayo NA, Wexler RR, Bolognesi ML, Ripka A, Young W. Blanco MJ, et al. Among authors: lagiakos hr. J Med Chem. 2024 Mar 28;67(6):4251-4258. doi: 10.1021/acs.jmedchem.4c00493. Epub 2024 Mar 8. J Med Chem. 2024. PMID: 38456628
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: lagiakos hr. 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.