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. 2021 Jan;2(1):3-5.
doi: 10.1038/s43018-020-00165-6.

A venetoclax bench-to-bedside story

Courtney D DiNardo  1 , Marina Y Konopleva  2
Affiliations

A venetoclax bench-to-bedside story

Courtney D DiNardo et al. Nat Cancer. 2021 Jan.
No abstract available

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Figures

Figure 1
Figure 1
At left is an overview of pro- and anti-apoptotic molecules. Venetoclax binds to BCL-2, which results in the release of BH3-only proteins that activate the executioner proteins BAX and BAK; this causes release of cytochrome c, disruption of the mitochondrial membrane, the formation of apoptosome complexes, caspase activation and apoptotic cell death. At right are the binding specificities of various BH3 mimetics to specific anti-apoptotic proteins (BCL-2, BCL-XL, BCL-W and MCL-1). ABT-737 and ABT-263 are first-generation BH3 mimetics that bind BCL-2, BCL-XL and BCL-W, whereas venetoclax (VEN) selectively binds BCL-2. Visual Art, University of Texas MD Anderson Cancer Center. © 2021.
See this image and copyright information in PMC

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