Abstract
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.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 17-22 |
| Number of pages | 6 |
| Journal | Drug Discovery Today: Technologies |
| Volume | 19 |
| DOIs | |
| State | Published - Mar 1 2016 |
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ASJC Scopus subject areas
- Biotechnology
- Molecular Medicine
- Drug Discovery
Cite this
Phospho-BRD4 : transcription plasticity and drug targeting. / Chiang, Cheng Ming.
In: Drug Discovery Today: Technologies, Vol. 19, 01.03.2016, p. 17-22.Research output: Contribution to journal › Review article
}
TY - JOUR
T1 - Phospho-BRD4
T2 - transcription plasticity and drug targeting
AU - Chiang, Cheng Ming
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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UR - http://www.scopus.com/inward/citedby.url?scp=84992392031&partnerID=8YFLogxK
U2 - 10.1016/j.ddtec.2016.05.003
DO - 10.1016/j.ddtec.2016.05.003
M3 - Review article
VL - 19
SP - 17
EP - 22
JO - Drug Discovery Today: Technologies
JF - Drug Discovery Today: Technologies
SN - 1740-6749
ER -