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World J Gastrointest Oncol. Jan 15, 2022; 14(1): 75-89
Published online Jan 15, 2022. doi: 10.4251/wjgo.v14.i1.75
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
Hui-Yan Sun, Song-Tao Du, Ya-Yun Li, Guang-Tong Deng, Fu-Rong Zeng, Department of Dermatology, Xiangya Hospital, Central South University, Changsha 410008, Hunan Province, China
Hui-Yan Sun, Fu-Rong Zeng, Department of Oncology, Xiangya Hospital, Central South University, Changsha 410008, Hunan Province, China
Hui-Yan Sun, Song-Tao Du, Ya-Yun Li, Guang-Tong Deng, Fu-Rong Zeng, Hunan Engineering Research Center of Skin Health and Disease, Hunan Key Laboratory of Skin Cancer and Psoriasis, Xiangya Hospital, Central South University, Changsha 410008, Hunan Province, China
Hui-Yan Sun, Song-Tao Du, Ya-Yun Li, Guang-Tong Deng, Fu-Rong Zeng, National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha 410008, Hunan Province, China
Song-Tao Du, Department of Colorectal Surgical Oncology, Harbin Medical University Cancer Hospital, Harbin 150081, Heilongjiang Province, China
Author contributions: Zeng FR, Deng GT and Sun HY designed the study; Sun HY and Deng GT wrote the manuscript; Du ST, Li YY helped to revise the manuscript; all the authors supported the study.
Supported by Fellowship of the China Postdoctoral Science Foundation, No. 2020M682594, and No. 2021T140748.
Conflict-of-interest statement: No conflict of interest.
Open-Access: This article is an open-access article that was selected by an in-house editor and fully peer-reviewed by external reviewers. It is distributed in accordance with the Creative Commons Attribution NonCommercial (CC BY-NC 4.0) license, which permits others to distribute, remix, adapt, build upon this work non-commercially, and license their derivative works on different terms, provided the original work is properly cited and the use is non-commercial. See: https://creativecommons.org/Licenses/by-nc/4.0/
Corresponding author: Fu-Rong Zeng, MD, Doctor, Department of Oncology, Xiangya Hospital, Central South University, No. 87 Xiangya Road, Changsha 410008, Hunan Province, China. zengflorachn@hotmail.com
Received: March 17, 2021
Peer-review started: March 17, 2021
First decision: July 27, 2021
Revised: August 11, 2021
Accepted: November 30, 2021
Article in press: November 30, 2021
Published online: January 15, 2022
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: Gastrointestinal cancer, Bromodomain and extra-terminal proteins, Bromodomain and extra-terminal inhibitors, Acetylated lysines

Core Tip: Bromodomain and extra-terminal (BET) inhibitors, as promising targeted agents, emerge as a new therapeutic avenue for gastrointestinal (GI) cancers. Based on preclinical evidence, BET inhibitors, alone or in combination with other therapies, were effective to suppress the progression of GI cancers.