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Discovery and biological characterization of potent myeloid cell leukemia-1 inhibitors.
- Source :
- FEBS Letters; Jan2017, Vol. 591 Issue 1, p240-251, 12p
- Publication Year :
- 2017
-
Abstract
- Myeloid cell leukemia 1 ( Mcl-1) is an antiapoptotic member of the Bcl-2 family of proteins that when overexpressed is associated with high tumor grade, poor survival, and resistance to chemotherapy. Mcl-1 is amplified in many human cancers, and knockdown of Mcl-1 using RNAi can lead to apoptosis. Thus, Mcl-1 is a promising cancer target. Here, we describe the discovery of picomolar Mcl-1 inhibitors that cause caspase activation, mitochondrial depolarization, and selective growth inhibition. These compounds represent valuable tools to study the role of Mcl-1 in cancer and serve as useful starting points for the discovery of clinically useful Mcl-1 inhibitors. PDB ID codes Comp. 2: ; Comp. 5: . [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 00145793
- Volume :
- 591
- Issue :
- 1
- Database :
- Complementary Index
- Journal :
- FEBS Letters
- Publication Type :
- Academic Journal
- Accession number :
- 120688924
- Full Text :
- https://doi.org/10.1002/1873-3468.12497