Mitochondrial apoptosis and BH3 mimetics

Haiming Dai; X. Wei Meng; Scott H. Kaufmann

doi:10.12688/f1000research.9629.1

Mitochondrial apoptosis and BH3 mimetics

Haiming Dai, X. Wei Meng, Scott H. Kaufmann

Oncology

Research output: Contribution to journal › Review article › peer-review

23 Scopus citations

Abstract

The BCL2-selective BH3 mimetic venetoclax was recently approved for the treatment of relapsed, chromosome 17p-deleted chronic lymphocytic leukemia (CLL) and is undergoing extensive testing, alone and in combination, in lymphomas, acute leukemias, and solid tumors. Here we summarize recent advances in understanding of the biology of BCL2 family members that shed light on the action of BH3 mimetics, review preclinical and clinical studies leading to the regulatory approval of venetoclax, and discuss future investigation of this new class of antineoplastic agent.

Original language	English (US)
Article number	2804
Journal	F1000Research
Volume	5
DOIs	https://doi.org/10.12688/f1000research.9629.1
State	Published - 2016

Keywords

BAK activation
BAX activation
BCL-2 inhibitors
BH3 mimetics
venetoclax

ASJC Scopus subject areas

General Immunology and Microbiology
General Pharmacology, Toxicology and Pharmaceutics
General Biochemistry, Genetics and Molecular Biology

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10.12688/f1000research.9629.1

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title = "Mitochondrial apoptosis and BH3 mimetics",

abstract = "The BCL2-selective BH3 mimetic venetoclax was recently approved for the treatment of relapsed, chromosome 17p-deleted chronic lymphocytic leukemia (CLL) and is undergoing extensive testing, alone and in combination, in lymphomas, acute leukemias, and solid tumors. Here we summarize recent advances in understanding of the biology of BCL2 family members that shed light on the action of BH3 mimetics, review preclinical and clinical studies leading to the regulatory approval of venetoclax, and discuss future investigation of this new class of antineoplastic agent.",

keywords = "BAK activation, BAX activation, BCL-2 inhibitors, BH3 mimetics, venetoclax",

author = "Haiming Dai and Meng, {X. Wei} and Kaufmann, {Scott H.}",

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T1 - Mitochondrial apoptosis and BH3 mimetics

AU - Dai, Haiming

AU - Meng, X. Wei

AU - Kaufmann, Scott H.

N1 - Publisher Copyright: ï¿½ 2016 Dai H et al.

PY - 2016

Y1 - 2016

N2 - The BCL2-selective BH3 mimetic venetoclax was recently approved for the treatment of relapsed, chromosome 17p-deleted chronic lymphocytic leukemia (CLL) and is undergoing extensive testing, alone and in combination, in lymphomas, acute leukemias, and solid tumors. Here we summarize recent advances in understanding of the biology of BCL2 family members that shed light on the action of BH3 mimetics, review preclinical and clinical studies leading to the regulatory approval of venetoclax, and discuss future investigation of this new class of antineoplastic agent.

AB - The BCL2-selective BH3 mimetic venetoclax was recently approved for the treatment of relapsed, chromosome 17p-deleted chronic lymphocytic leukemia (CLL) and is undergoing extensive testing, alone and in combination, in lymphomas, acute leukemias, and solid tumors. Here we summarize recent advances in understanding of the biology of BCL2 family members that shed light on the action of BH3 mimetics, review preclinical and clinical studies leading to the regulatory approval of venetoclax, and discuss future investigation of this new class of antineoplastic agent.

KW - BAK activation

KW - BAX activation

KW - BCL-2 inhibitors

KW - BH3 mimetics

KW - venetoclax

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VL - 5

JO - F1000Research

JF - F1000Research

M1 - 2804

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Mitochondrial apoptosis and BH3 mimetics

Abstract

Keywords

ASJC Scopus subject areas

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