Bromodomain and extra-terminal inhibitors emerge as potential therapeutic avenues for gastrointestinal cancers

Hui-Yan Sun; Song-Tao Du; Ya-Yun Li; Guang-Tong Deng; Fu-Rong Zeng

doi:10.4251/wjgo.v14.i1.75

Bromodomain and extra-terminal inhibitors emerge as potential therapeutic avenues for gastrointestinal cancers

World J Gastrointest Oncol. 2022 Jan 15;14(1):75-89. doi: 10.4251/wjgo.v14.i1.75.

Authors

Hui-Yan Sun¹, Song-Tao Du¹, Ya-Yun Li¹, Guang-Tong Deng¹, Fu-Rong Zeng¹

Affiliation

¹ Department of Dermatology, Xiangya Hospital, Central South University, Changsha 410008, Hunan Province, China.

Abstract

Gastrointestinal (GI) cancers, including colorectal cancer, pancreatic cancer, liver cancer and gastric cancer, are severe social burdens due to high incidence and mortality rates. Bromodomain and extra-terminal (BET) proteins are epigenetic readers consisting of four conserved members (BRD2, BRD3, BRD4 and BRDT). BET family perform pivotal roles in tumorigenesis through transcriptional regulation, thereby emerging as potential therapeutic targets. BET inhibitors, disrupting the interaction between BET proteins and acetylated lysines, have been reported to suppress tumor initiation and progression in most of GI cancers. In this review, we will demonstrate how BET proteins participate in the GI cancers progression and highlight the therapeutic potential of targeting BET proteins for GI cancers treatment.

Keywords: Acetylated lysines; Bromodomain and extra-terminal inhibitors; Bromodomain and extra-terminal proteins; Gastrointestinal cancer.

Publication types

Review