Precision Targeting of BET Proteins - Navigating Disease Pathways, Inhibitor Insights, and Shaping Therapeutic Frontiers: A Comprehensive Review.

IF 3 4区 医学 Q2 PHARMACOLOGY & PHARMACY Current drug targets Pub Date : 2024-10-08 DOI:10.2174/0113894501304747240823111337
Rakesh D Amrutkar, Mehul V Amesar, Lokesh B Chavan, Nilesh S Baviskar, Vaibhav B Bhamare
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Abstract

The family of proteins known as Bromodomain and Extra-Terminal (BET) proteins has become a key participant in the control of gene expression, having a significant impact on numerous physiological and pathological mechanisms. This review offers a thorough investigation of the BET protein family, clarifying its various roles in essential cellular processes and its connection to a variety of illnesses, from inflammatory disorders to cancer. The article explores the structural and functional features of BET proteins, emphasizing their special bromodomain modules that control chromatin dynamics by identifying acetylated histones. BET proteins' complex roles in the development of cardiovascular, neurodegenerative, and cancer diseases are carefully investigated, providing insight into possible treatment avenues. In addition, the review carefully examines the history and relevance of BET inhibitors, demonstrating their capacity to modify gene expression profiles and specifically target BET proteins. The encouraging outcomes of preclinical and clinical research highlight BET inhibitors' therapeutic potential across a range of disease contexts. The article summarizes the state of BET inhibitors today and makes predictions about the challenges and future directions of the field. This article provides insights into the changing field of BET protein-targeted interventions by discussing the potential of personalized medicine and combination therapies involving BET inhibitors. This thorough analysis combines many aspects of BET proteins, such as their physiological roles and their roles in pathophysiological conditions. As such, it is an invaluable tool for scientists and medical professionals who are trying to figure out how to treat patients by using this fascinating protein family.

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BET 蛋白的精准靶向--疾病途径导航、抑制剂洞察力和治疗前沿的塑造:全面回顾。
Bromodomain and Extra-Terminal (BET) 蛋白家族已成为控制基因表达的关键参与者,对许多生理和病理机制产生了重大影响。这篇综述对 BET 蛋白家族进行了深入研究,阐明了它在重要细胞过程中的各种作用,以及它与从炎症性疾病到癌症等各种疾病的联系。文章探讨了 BET 蛋白的结构和功能特点,强调了其特殊的溴域模块,该模块通过识别乙酰化组蛋白来控制染色质动力学。文章仔细研究了 BET 蛋白在心血管疾病、神经退行性疾病和癌症发展过程中的复杂作用,为可能的治疗途径提供了启示。此外,综述还仔细研究了 BET 抑制剂的历史和相关性,展示了它们改变基因表达谱和特异性靶向 BET 蛋白的能力。临床前和临床研究取得的令人鼓舞的成果凸显了 BET 抑制剂在各种疾病中的治疗潜力。文章总结了 BET 抑制剂目前的发展状况,并预测了该领域面临的挑战和未来的发展方向。本文通过讨论个性化医疗和涉及 BET 抑制剂的联合疗法的潜力,深入探讨了不断变化的 BET 蛋白靶向干预领域。这篇详尽的分析结合了 BET 蛋白的许多方面,如其生理作用及其在病理生理条件下的作用。因此,对于那些试图找出如何利用这个迷人的蛋白家族来治疗病人的科学家和医学专家来说,这是一本非常有价值的工具书。
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来源期刊
Current drug targets
Current drug targets 医学-药学
CiteScore
6.20
自引率
0.00%
发文量
127
审稿时长
3-8 weeks
期刊介绍: Current Drug Targets aims to cover the latest and most outstanding developments on the medicinal chemistry and pharmacology of molecular drug targets e.g. disease specific proteins, receptors, enzymes, genes. Current Drug Targets publishes guest edited thematic issues written by leaders in the field covering a range of current topics of drug targets. The journal also accepts for publication mini- & full-length review articles and drug clinical trial studies. As the discovery, identification, characterization and validation of novel human drug targets for drug discovery continues to grow; this journal is essential reading for all pharmaceutical scientists involved in drug discovery and development.
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