The application of PROTACs in immune-inflammation diseases

IF 3.3 3区医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Bioorganic & Medicinal Chemistry Pub Date : 2024-10-26 DOI:10.1016/j.bmc.2024.117967

Chao Zhang , Xiuyun Sun , Peilu Song , Yu Rao

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Abstract

Immune-inflammatory diseases are a class of conditions with high prevalence that severely impact the quality of life. Current treatment strategies include immunosuppressants, glucocorticoids, and monoclonal antibodies. However, these approaches have certain limitations, such as poor membrane permeability, immunogenicity, and the requirement for injection in large molecule drugs. Small molecule compounds, on the other hand, suffer from issues like poor selectivity, inability to inhibit non-enzymatic functions, and biological compensation. These factors constrain the effectiveness of current therapeutic strategies in immune-inflammatory diseases. As a novel small molecule drug development technology, proteolysis-targeting chimeras (PROTACs) regulate protein levels by inducing interactions between target proteins and E3 ubiquitin ligases, leading to the selective degradation of target proteins. This technology has already shown promising therapeutic effects in the treatment of immune-inflammatory diseases. This review aims to comprehensively summarize the application of PROTAC technology in the field of immune inflammation and provide insights into its potential in treating immune-inflammatory diseases.

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PROTAC 在免疫炎症疾病中的应用

免疫炎症性疾病是一类发病率很高的疾病，严重影响患者的生活质量。目前的治疗策略包括免疫抑制剂、糖皮质激素和单克隆抗体。然而，这些方法都有一定的局限性，如膜渗透性差、免疫原性以及大分子药物需要注射等。而小分子化合物则存在选择性差、无法抑制非酶功能和生物补偿等问题。这些因素制约了当前免疫炎症性疾病治疗策略的有效性。作为一种新型小分子药物开发技术，蛋白水解靶向嵌合体（PROTACs）通过诱导靶蛋白与 E3 泛素连接酶之间的相互作用来调节蛋白水平，从而导致靶蛋白的选择性降解。这项技术在治疗免疫炎症性疾病方面已显示出良好的治疗效果。本综述旨在全面总结 PROTAC 技术在免疫炎症领域的应用，并深入探讨其在治疗免疫炎症疾病方面的潜力。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Bioorganic & Medicinal Chemistry 医学-生化与分子生物学

CiteScore

6.80

自引率

2.90%

发文量

413

审稿时长

17 days

期刊介绍： Bioorganic & Medicinal Chemistry provides an international forum for the publication of full original research papers and critical reviews on molecular interactions in key biological targets such as receptors, channels, enzymes, nucleotides, lipids and saccharides. The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction of these with chemical agents. A special feature will be that colour illustrations will be reproduced at no charge to the author, provided that the Editor agrees that colour is essential to the information content of the illustration in question.