TY - JOUR
T1 - Phospho-BRD4
T2 - transcription plasticity and drug targeting
AU - Chiang, Cheng Ming
N1 - Funding Information:
I thank Dr. Shwu-Yuan Wu for illustration and discussion. Research in my lab is currently supported by grants from the National Institutes of Health ( CA103867 ), Cancer Prevention Research Institute of Texas ( RP110471 and RP140367 ), and the Welch Foundation ( I-1805 ).
Publisher Copyright:
© 2016 Elsevier Ltd
Copyright:
Copyright 2017 Elsevier B.V., All rights reserved.
PY - 2016/3/1
Y1 - 2016/3/1
N2 - BRD4 is an epigenetic regulator and transcription cofactor whose phosphorylation by CK2 and dephosphorylation by PP2A modulates its function in chromatin targeting, factor recruitment, and cancer progression. While the bromodomains of BET family proteins, including BRD4, BRD2, BRD3 and BRDT, have been the primary targets of small compounds such as JQ1, I-BET and MS417 that show promising anticancer effects against some hematopoietic cancer and solid tumors, drug resistance upon prolonged treatment necessitates a better understanding of alternative pathways underlying not only the resistance but also persistent BET protein dependence for identifying new targets and effective combination therapy strategies.
AB - BRD4 is an epigenetic regulator and transcription cofactor whose phosphorylation by CK2 and dephosphorylation by PP2A modulates its function in chromatin targeting, factor recruitment, and cancer progression. While the bromodomains of BET family proteins, including BRD4, BRD2, BRD3 and BRDT, have been the primary targets of small compounds such as JQ1, I-BET and MS417 that show promising anticancer effects against some hematopoietic cancer and solid tumors, drug resistance upon prolonged treatment necessitates a better understanding of alternative pathways underlying not only the resistance but also persistent BET protein dependence for identifying new targets and effective combination therapy strategies.
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U2 - 10.1016/j.ddtec.2016.05.003
DO - 10.1016/j.ddtec.2016.05.003
M3 - Review article
C2 - 27769352
AN - SCOPUS:84992392031
VL - 19
SP - 17
EP - 22
JO - Drug Discovery Today: Technologies
JF - Drug Discovery Today: Technologies
SN - 1740-6749
ER -