AMG 176, a Selective MCL1 Inhibitor, Is Effective in Hematologic Cancer Models Alone and in Combination with Established Therapies

Caenepeel, Sean; P. Brown, Sean; Belmontes, Brian; Moody, Gordon; S. Keegan, Kathleen; Chui, Danny; A. Whittington, Douglas; Huang, Xin; Poppe, Leszek; C. Cheng, Alan; Cardozo, Mario; B. Houze, Jonathan; Li, Yunxiao; S. Lucas, Brian; A. Paras, Nick; Wang, Xianghong; P. Taygerly, Joshua; Vimolratana, Marc; Zancanella, Manuel; Zhu, Liusheng; Cajulis, Elaina; Osgood, Tao; Sun, Jan; J. Damon, Leah; K. Egan, Regina; Greninger, Patricia; McClanaghan, Joseph; Gong, Jianan; M. Moujalled, Donia; Pomilio, Giovanna; J. Beltran, Pedro; H. Benes, Cyril; W. Roberts, Andrew; C.S. Huang, David; H. Wei, Andrew; Canon, Jude; Coxon, Angela; E. Hughes, Paul

doi:10.1158/2159-8290.cd-18-0387

Public

AMG 176, a Selective MCL1 Inhibitor, Is Effective in Hematologic Cancer Models Alone and in Combination with Established Therapies

Published in Cancer Discovery • Sep 25, 2018

Authors:

Sean Caenepeel

Sean P. Brown

Brian Belmontes

Abstract

Abstract The prosurvival BCL2 family member MCL1 is frequently dysregulated in cancer. To overcome the significant challenges associated with inhibition of MCL1 protein–protein interactions, we rigorously applied small-molecule conformational restriction, which culminated in the discovery of AMG 176...

Subject

MCL1

Cancer

Hematologic Neoplasms

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