Targeting bet bromodomain proteins in solid tumors

Vaibhav Sahai; Amanda J. Redig; Katharine A. Collier; Frank D. Eckerdt; Hidayatullah G. Munshi

doi:10.18632/oncotarget.9804

Targeting bet bromodomain proteins in solid tumors

Vaibhav Sahai, Amanda J. Redig, Katharine A. Collier, Frank D. Eckerdt, Hidayatullah G. Munshi^*

^*Corresponding author for this work

Medicine, Hematology Oncology Division

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

85 Scopus citations

Abstract

There is increasing interest in inhibitors targeting BET (bromodomain and extraterminal) proteins because of the association between this family of proteins and cancer progression. BET inhibitors were initially shown to have efficacy in hematologic malignancies; however, a number of studies have now shown that BET inhibitors can also block progression of non-hematologic malignancies. In this Review, we summarize the efficacy of BET inhibitors in select solid tumors; evaluate the role of BET proteins in mediating resistance to current targeted therapies; and consider potential toxicities of BET inhibitors. We also evaluate recently characterized mechanisms of resistance to BET inhibitors; summarize ongoing clinical trials with these inhibitors; and discuss potential future roles of BET inhibitors in patients with solid tumors.

Original language	English (US)
Pages (from-to)	53997-54009
Number of pages	13
Journal	Oncotarget
Volume	7
Issue number	33
DOIs	https://doi.org/10.18632/oncotarget.9804
State	Published - Aug 1 2016

Funding

Keywords

Brain tumors
Breast and prostate cancers
Gastrointestinal cancers
Lung cancers
NUT midline carcinoma

ASJC Scopus subject areas

Oncology

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.18632/oncotarget.9804

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title = "Targeting bet bromodomain proteins in solid tumors",

abstract = "There is increasing interest in inhibitors targeting BET (bromodomain and extraterminal) proteins because of the association between this family of proteins and cancer progression. BET inhibitors were initially shown to have efficacy in hematologic malignancies; however, a number of studies have now shown that BET inhibitors can also block progression of non-hematologic malignancies. In this Review, we summarize the efficacy of BET inhibitors in select solid tumors; evaluate the role of BET proteins in mediating resistance to current targeted therapies; and consider potential toxicities of BET inhibitors. We also evaluate recently characterized mechanisms of resistance to BET inhibitors; summarize ongoing clinical trials with these inhibitors; and discuss potential future roles of BET inhibitors in patients with solid tumors.",

keywords = "Brain tumors, Breast and prostate cancers, Gastrointestinal cancers, Lung cancers, NUT midline carcinoma",

author = "Vaibhav Sahai and Redig, {Amanda J.} and Collier, {Katharine A.} and Eckerdt, {Frank D.} and Munshi, {Hidayatullah G.}",

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T1 - Targeting bet bromodomain proteins in solid tumors

AU - Sahai, Vaibhav

AU - Redig, Amanda J.

AU - Collier, Katharine A.

AU - Eckerdt, Frank D.

AU - Munshi, Hidayatullah G.

PY - 2016/8/1

Y1 - 2016/8/1

N2 - There is increasing interest in inhibitors targeting BET (bromodomain and extraterminal) proteins because of the association between this family of proteins and cancer progression. BET inhibitors were initially shown to have efficacy in hematologic malignancies; however, a number of studies have now shown that BET inhibitors can also block progression of non-hematologic malignancies. In this Review, we summarize the efficacy of BET inhibitors in select solid tumors; evaluate the role of BET proteins in mediating resistance to current targeted therapies; and consider potential toxicities of BET inhibitors. We also evaluate recently characterized mechanisms of resistance to BET inhibitors; summarize ongoing clinical trials with these inhibitors; and discuss potential future roles of BET inhibitors in patients with solid tumors.

AB - There is increasing interest in inhibitors targeting BET (bromodomain and extraterminal) proteins because of the association between this family of proteins and cancer progression. BET inhibitors were initially shown to have efficacy in hematologic malignancies; however, a number of studies have now shown that BET inhibitors can also block progression of non-hematologic malignancies. In this Review, we summarize the efficacy of BET inhibitors in select solid tumors; evaluate the role of BET proteins in mediating resistance to current targeted therapies; and consider potential toxicities of BET inhibitors. We also evaluate recently characterized mechanisms of resistance to BET inhibitors; summarize ongoing clinical trials with these inhibitors; and discuss potential future roles of BET inhibitors in patients with solid tumors.

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KW - Breast and prostate cancers

KW - Gastrointestinal cancers

KW - Lung cancers

KW - NUT midline carcinoma

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Targeting bet bromodomain proteins in solid tumors

Abstract

Funding

Keywords

ASJC Scopus subject areas

UN SDGs

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