Identification of an Imidazopyridine-based Compound as an Oral Selective Estrogen Receptor Degrader for Breast Cancer Therapy

鉴定一种咪唑并吡啶类化合物作为乳腺癌治疗的口服选择性雌激素受体降解剂

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作者:Mengwu Pan #, Valeria Solozobova #, Nane C Kuznik, Nicole Jung, Simone Gräßle, Victor Gourain, Yvonne M Heneka, Christina A Cramer von Clausbruch, Olaf Fuhr, Ravi S N Munuganti, Danilo Maddalo, Christine Blattner, Antje Neeb, Adam Sharp, Laura Cato, Carsten Weiss, Rinath M Jeselsohn, Veronique Orian

Significance

An imidazopyridine that selectively degrades ERα and is orally bioavailable has been identified for the development of ER+ breast cancer therapeutics. This compound also activates wild-type p53 and disrupts the gain-of-function tumorigenic activity of mutant p53, resulting in cell-cycle arrest and the induction of apoptosis.

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