American Association for Cancer Research
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Figure S1 from Identification of an Imidazopyridine-based Compound as an Oral Selective Estrogen Receptor Degrader for Breast Cancer Therapy

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posted on 2023-07-27, 14:20 authored by 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-Rousseau, Stefan Bräse, Andrew C. B. Cato

Volcano plots and Hallmark gene set analyses showing pathways targeted by X15695.

Funding

Wilhelm Sander-Stiftung (Wilhelm Sander Foundation)

China Scholarship Council (CSC)

Prostate Cancer UK (Prostate Cancer)

History

ARTICLE ABSTRACT

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.