Fragment-based discovery of potent inhibitors of the anti-apoptotic MCL-1 protein

AM Petros, SL Swann, D Song, K Swinger…

Index: Petros, Andrew M.; Swann, Steven L.; Song, Danying; Swinger, Kerren; Park, Chang; Zhang, Haichao; Wendt, Michael D.; Kunzer, Aaron R.; Souers, Andrew J.; Sun, Chaohong Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 6 p. 1484 - 1488

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Citation Number: 42

Abstract

Abstract Apoptosis is regulated by the BCL-2 family of proteins, which is comprised of both pro-death and pro-survival members. Evasion of apoptosis is a hallmark of malignant cells. One way in which cancer cells achieve this evasion is thru overexpression of the pro- survival members of the BCL-2 family. Overexpression of MCL-1, a pro-survival protein, has been shown to be a resistance factor for Navitoclax, a potent inhibitor of BCL-2 and BCL- ...