Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia

Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia

High expression of Mcl-1 promotes tumorigenesis and resistance to anticancer therapies. Here they report a macrocyclic molecule with high selectivity and affinity for Mcl-1 that exhibits potent anti-tumor effects as single agent and in combination with bortezomib or venetoclax in preclinical models...

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Bibliographic Details
Main Authors: Adriana E. Tron, Matthew A. Belmonte, Ammar Adam, Brian M. Aquila, Lawrence H. Boise, Elisabetta Chiarparin, Justin Cidado, Kevin J. Embrey, Eric Gangl, Francis D. Gibbons, Gareth P. Gregory, David Hargreaves, J. Adam Hendricks, Jeffrey W. Johannes, Ricky W. Johnstone, Steven L. Kazmirski, Jason G. Kettle, Michelle L. Lamb, Shannon M. Matulis, Ajay K. Nooka, Martin J. Packer, Bo Peng, Philip B. Rawlins, Daniel W. Robbins, Alwin G. Schuller, Nancy Su, Wenzhan Yang, Qing Ye, Xiaolan Zheng, J. Paul Secrist, Edwin A. Clark, David M. Wilson, Stephen E. Fawell, Alexander W. Hird
Format: Article
Language:English
Published: Nature Publishing Group 2018-12-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-018-07551-w

Internet

https://doi.org/10.1038/s41467-018-07551-w

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