Abstract
Venetoclax is a BH3 mimetic approved for treating chronic lymphocytic leukemia. Cancer cells are resistant to apoptosis but "primed for death" by elevated BCL-2, which binds to pro-apoptotic proteins and holds them in check. Venetoclax releases this antagonism and is the first approved drug to target a protein-protein interaction.
Copyright © 2016. Published by Elsevier Inc.
MeSH terms
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Antineoplastic Agents / therapeutic use*
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Apoptosis / drug effects
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Apoptosis Regulatory Proteins / antagonists & inhibitors
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Apoptosis Regulatory Proteins / metabolism
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Bridged Bicyclo Compounds, Heterocyclic / therapeutic use*
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Drug Approval*
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Humans
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Leukemia, Lymphocytic, Chronic, B-Cell / drug therapy*
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Proto-Oncogene Proteins c-bcl-2 / antagonists & inhibitors
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Proto-Oncogene Proteins c-bcl-2 / metabolism
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Sulfonamides / therapeutic use*
Substances
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Antineoplastic Agents
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Apoptosis Regulatory Proteins
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BCL2 protein, human
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Bridged Bicyclo Compounds, Heterocyclic
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Proto-Oncogene Proteins c-bcl-2
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Sulfonamides
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venetoclax