Venkatesan Janarthanan, Murugan Dhanashree, Rangasamy Loganathan
Drug Discovery Unit (DDU), Centre for Biomaterials, Cellular, and Molecular Theranostics (CBCMT), Vellore Institute of Technology (VIT), Vellore 632014, Tamil Nadu, India.
School of Advanced Sciences (SAS), Vellore Institute of Technology (VIT), Vellore 632014, Tamil Nadu, India.
Antibiotics (Basel). 2022 Nov 29;11(12):1717. doi: 10.3390/antibiotics11121717.
Targeted protein degradation is a new aspect in the field of drug discovery. Traditionally, developing an antibiotic includes tedious and expensive processes, such as drug screening, lead optimization, and formulation. Proteolysis-targeting chimeras (PROTACs) are new-generation drugs that use the proteolytic mechanism to selectively degrade and eliminate proteins involved in human diseases. The application of PROTACs is explored immensely in the field of cancer, and various PROTACs are in clinical trials. Thus, researchers have a profound interest in pursuing PROTAC technology as a new weapon to fight pathogenic viruses and bacteria. This review highlights the importance of antimicrobial PROTACs and other similar "PROTAC-like" techniques to degrade pathogenic target proteins (i.e., viral/bacterial proteins). These techniques can perform specific protein degradation of the pathogenic protein to avoid resistance caused by mutations or abnormal expression of the pathogenic protein. PROTAC-based antimicrobial therapeutics have the advantage of high specificity and the ability to degrade "undruggable" proteins, such as nonenzymatic and structural proteins.
靶向蛋白质降解是药物研发领域的一个新方向。传统上,开发一种抗生素需要繁琐且昂贵的过程,如药物筛选、先导化合物优化和制剂研发。蛋白酶靶向嵌合体(PROTACs)是新一代药物,其利用蛋白水解机制选择性地降解和消除与人类疾病相关的蛋白质。PROTACs在癌症领域得到了广泛的应用探索,多种PROTACs正在进行临床试验。因此,研究人员对将PROTAC技术作为对抗致病病毒和细菌的新武器有着浓厚的兴趣。这篇综述强调了抗菌PROTACs以及其他类似的“类PROTAC”技术在降解致病靶蛋白(即病毒/细菌蛋白)方面的重要性。这些技术能够对致病蛋白进行特异性的蛋白质降解,以避免因致病蛋白突变或异常表达而产生的耐药性。基于PROTAC的抗菌疗法具有高特异性以及能够降解“不可成药”蛋白质(如非酶蛋白和结构蛋白)的优势。