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Roles of Bromodomain Extra Terminal Proteins in Metabolic Signaling and Diseases
BET proteins, which recognize and bind to acetylated histones, play a key role in transcriptional regulation. The development of chemical BET inhibitors in 2010 greatly facilitated the study of these proteins. BETs play crucial roles in cancer, inflammation, heart failure, and fibrosis. In particula...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9414451/ https://www.ncbi.nlm.nih.gov/pubmed/36015180 http://dx.doi.org/10.3390/ph15081032 |
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author | Wu, Dayu Duan, Qiong |
author_facet | Wu, Dayu Duan, Qiong |
author_sort | Wu, Dayu |
collection | PubMed |
description | BET proteins, which recognize and bind to acetylated histones, play a key role in transcriptional regulation. The development of chemical BET inhibitors in 2010 greatly facilitated the study of these proteins. BETs play crucial roles in cancer, inflammation, heart failure, and fibrosis. In particular, BETs may be involved in regulating metabolic processes, such as adipogenesis and metaflammation, which are under tight transcriptional regulation. In addition, acetyl-CoA links energy metabolism with epigenetic modification through lysine acetylation, which creates docking sites for BET. Given this, it is possible that the ambient energy status may dictate metabolic gene transcription via a BET-dependent mechanism. Indeed, recent studies have reported that various BET proteins are involved in both metabolic signaling regulation and disease. Here, we discuss some of the most recent information on BET proteins and their regulation of the metabolism in both cellular and animal models. Further, we summarize data from some randomized clinical trials evaluating BET inhibitors for the treatment of metabolic diseases. |
format | Online Article Text |
id | pubmed-9414451 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-94144512022-08-27 Roles of Bromodomain Extra Terminal Proteins in Metabolic Signaling and Diseases Wu, Dayu Duan, Qiong Pharmaceuticals (Basel) Review BET proteins, which recognize and bind to acetylated histones, play a key role in transcriptional regulation. The development of chemical BET inhibitors in 2010 greatly facilitated the study of these proteins. BETs play crucial roles in cancer, inflammation, heart failure, and fibrosis. In particular, BETs may be involved in regulating metabolic processes, such as adipogenesis and metaflammation, which are under tight transcriptional regulation. In addition, acetyl-CoA links energy metabolism with epigenetic modification through lysine acetylation, which creates docking sites for BET. Given this, it is possible that the ambient energy status may dictate metabolic gene transcription via a BET-dependent mechanism. Indeed, recent studies have reported that various BET proteins are involved in both metabolic signaling regulation and disease. Here, we discuss some of the most recent information on BET proteins and their regulation of the metabolism in both cellular and animal models. Further, we summarize data from some randomized clinical trials evaluating BET inhibitors for the treatment of metabolic diseases. MDPI 2022-08-22 /pmc/articles/PMC9414451/ /pubmed/36015180 http://dx.doi.org/10.3390/ph15081032 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Wu, Dayu Duan, Qiong Roles of Bromodomain Extra Terminal Proteins in Metabolic Signaling and Diseases |
title | Roles of Bromodomain Extra Terminal Proteins in Metabolic Signaling and Diseases |
title_full | Roles of Bromodomain Extra Terminal Proteins in Metabolic Signaling and Diseases |
title_fullStr | Roles of Bromodomain Extra Terminal Proteins in Metabolic Signaling and Diseases |
title_full_unstemmed | Roles of Bromodomain Extra Terminal Proteins in Metabolic Signaling and Diseases |
title_short | Roles of Bromodomain Extra Terminal Proteins in Metabolic Signaling and Diseases |
title_sort | roles of bromodomain extra terminal proteins in metabolic signaling and diseases |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9414451/ https://www.ncbi.nlm.nih.gov/pubmed/36015180 http://dx.doi.org/10.3390/ph15081032 |
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