Covalent ERα Antagonist H3B-6545 Demonstrates Encouraging Preclinical Activity in Therapy-Resistant Breast Cancer.
Craig FurmanXiaoling PuyangZhaojie ZhangZhenhua J WuDeepti BankaKiran B AithalLee A AlbackerMing-Hong HaoSean IrwinAmy KimMeagan MontesionAlyssa D MoriartyKarthikeyan MurugesanTuong-Vi NguyenVictoria RimkunasTarek SahmoudMichael J WickShihua YaoXun ZhangHao ZengFrédéric H VaillancourtDavid M BolducNicholas LarsenGuo Zhu ZhengSudeep PrajapatiPing ZhuManav KorpalPublished in: Molecular cancer therapeutics (2022)
H3B-6545 is an ERα covalent antagonist that exhibits encouraging preclinical activity against CDK4/6i naïve and resistant ERαWT and ERαMUT tumors.