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Comment
. 2023 Oct 19;30(10):1183-1185.
doi: 10.1016/j.chembiol.2023.08.006.

HATS off to KAT6A/B inhibitors: A new way to target estrogen-receptor-positive breast cancer

Rinath Jeselsohn  1 , Kornelia Polyak  2
Affiliations
Free article
Comment

HATS off to KAT6A/B inhibitors: A new way to target estrogen-receptor-positive breast cancer

Rinath Jeselsohn et al. Cell Chem Biol. .
Free article

Abstract

Inhibitors for the KAT6 family of histone acetyltransferases (HATs) have been actively pursued due to the oncogenic roles of KAT6A in human cancer. CTx-648 is a novel KAT6A/B inhibitor with excellent pharmacokinetic properties and in vivo efficacy that represents a promising new treatment strategy for estrogen-receptor-positive breast cancer.

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Conflict of interest statement

Declaration of interests The authors declare competing financial interests: K.P. serves on the scientific advisory board of Novartis, Vividion Therapeutics, Ideya Biosciences, and Scorpion Therapeutics; holds equity options in Scorpion Therapeutics and Ideya Biosciences; and receives sponsored research funding through Dana-Farber from Novartis. R.J. received research funding (institutional) from Pfizer and Lilly and is a consultant for Carrick Therapeutics and GE Health.

Comment on

  • 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. 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

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