TY - JOUR
T1 - Targeting BRD4
T2 - Potential therapeutic strategy for head and neck squamous cell carcinoma (Review)
AU - Yongprayoon, Voraporn
AU - Wattanakul, Napasporn
AU - Khomate, Winnada
AU - Apithanangsiri, Nathakrit
AU - Kasitipradit, Tarathip
AU - Nantajit, Danupon
AU - Tavassoli, Mahvash
N1 - Publisher Copyright:
Copyright © 2024 Yongprayoon et al.
PY - 2024/6
Y1 - 2024/6
N2 - As a member of BET (bromodomain and extraterminal) protein family, BRD4 (bromodomain-containing protein 4) is a chromatin-associated protein that interacts with acetylated histones and actively recruits regulatory proteins, leading to the modulation of gene expression and chromatin remodeling. The cellular and epigenetic functions of BRD4 implicate normal development, fibrosis and inflammation. BRD4 has been suggested as a potential therapeutic target as it is often overexpressed and plays a critical role in regulating gene expression programs that drive tumor cell proliferation, survival, migration and drug resistance. To address the roles of BRD4 in cancer, several drugs that specifically target BRD4 have been developed. Inhibition of BRD4 has shown promising results in preclinical models, with several BRD4 inhibitors undergoing clinical trials for the treatment of various cancers. Head and neck squamous cell carcinoma (HNSCC), a heterogeneous group of cancers, remains a health challenge with a high incidence rate and poor prognosis. Conventional therapies for HNSCC often cause adverse effects to the patients. Targeting BRD4, therefore, represents a promising strategy to sensitize HNSCC to chemo- and radiotherapy allowing de‑intensification of the current therapeutic regime and subsequent reduced side effects. However, further studies are required to fully understand the underlying mechanisms of action of BRD4 in HNSCC in order to determine the optimal dosing and administration of BRD4-targeted drugs for the treatment of patients with HNSCC.
AB - As a member of BET (bromodomain and extraterminal) protein family, BRD4 (bromodomain-containing protein 4) is a chromatin-associated protein that interacts with acetylated histones and actively recruits regulatory proteins, leading to the modulation of gene expression and chromatin remodeling. The cellular and epigenetic functions of BRD4 implicate normal development, fibrosis and inflammation. BRD4 has been suggested as a potential therapeutic target as it is often overexpressed and plays a critical role in regulating gene expression programs that drive tumor cell proliferation, survival, migration and drug resistance. To address the roles of BRD4 in cancer, several drugs that specifically target BRD4 have been developed. Inhibition of BRD4 has shown promising results in preclinical models, with several BRD4 inhibitors undergoing clinical trials for the treatment of various cancers. Head and neck squamous cell carcinoma (HNSCC), a heterogeneous group of cancers, remains a health challenge with a high incidence rate and poor prognosis. Conventional therapies for HNSCC often cause adverse effects to the patients. Targeting BRD4, therefore, represents a promising strategy to sensitize HNSCC to chemo- and radiotherapy allowing de‑intensification of the current therapeutic regime and subsequent reduced side effects. However, further studies are required to fully understand the underlying mechanisms of action of BRD4 in HNSCC in order to determine the optimal dosing and administration of BRD4-targeted drugs for the treatment of patients with HNSCC.
KW - bromodomain-containing protein 4
KW - de-escalation
KW - head and neck squamous cell carcinoma
KW - sensitization
KW - targeted therapy
UR - http://www.scopus.com/inward/record.url?scp=85190493168&partnerID=8YFLogxK
U2 - 10.3892/or.2024.8733
DO - 10.3892/or.2024.8733
M3 - Review article
C2 - 38606512
AN - SCOPUS:85190493168
SN - 1021-335X
VL - 51
JO - ONCOLOGY REPORTS
JF - ONCOLOGY REPORTS
IS - 6
M1 - 74
ER -
