Presloid Christopher J, Jiang Jialiu, Kandel Pratistha, Anderson Henry R, Beardslee Patrick C, Swayne Thomas M, Schmitz Karl R
Department of Biological Sciences, University of Delaware, Newark, Delaware, USA.
Department of Chemistry & Biochemistry, University of Delaware, Newark, Delaware, USA.
Mol Microbiol. 2025 Jan;123(1):16-30. doi: 10.1111/mmi.15334. Epub 2024 Dec 3.
Drug-resistant tuberculosis infections are a major threat to global public health. The essential mycobacterial ClpC1P1P2 protease has received attention as a prospective target for novel antibacterial therapeutics. However, efforts to probe its function in cells are constrained by our limited knowledge of its physiological proteolytic repertoire. Here, we interrogate the role of mycobacterial ClpS in directing N-degron pathway proteolysis by ClpC1P1P2 in Mycolicibacterium smegmatis. Binding assays demonstrate that mycobacterial ClpS binds canonical primary destabilizing residues (Leu, Phe, Tyr, Trp) with moderate affinity. N-degron binding restricts the conformational flexibility of a loop adjacent to the ClpS N-degron binding pocket and strengthens ClpS•ClpC1 binding affinity ~30-fold, providing a mechanism for cells to prioritize N-degron proteolysis when substrates are abundant. Proteolytic reporter assays in M. smegmatis confirm degradation of substrates bearing primary N-degrons, but suggest that secondary N-degrons are absent in mycobacteria. This work expands our understanding of the mycobacterial N-degron pathway and identifies ClpS as a critical component for substrate specificity, providing insights that may support the development of improved Clp protease inhibitors.
耐药结核病感染是对全球公共卫生的重大威胁。重要的分枝杆菌ClpC1P1P2蛋白酶作为新型抗菌治疗药物的潜在靶点受到关注。然而,由于我们对其生理蛋白水解谱的了解有限,探究其在细胞中的功能受到限制。在这里,我们研究了分枝杆菌ClpS在耻垢分枝杆菌中指导ClpC1P1P2进行N-端规则途径蛋白水解中的作用。结合实验表明,分枝杆菌ClpS以中等亲和力结合典型的主要不稳定残基(亮氨酸、苯丙氨酸、酪氨酸、色氨酸)。N-端规则结合限制了与ClpS N-端规则结合口袋相邻的环的构象灵活性,并将ClpS•ClpC1结合亲和力提高了约30倍,为细胞在底物丰富时优先进行N-端规则蛋白水解提供了一种机制。耻垢分枝杆菌中的蛋白水解报告基因实验证实了带有主要N-端规则的底物的降解,但表明分枝杆菌中不存在次要N-端规则。这项工作扩展了我们对分枝杆菌N-端规则途径的理解,并将ClpS鉴定为底物特异性的关键组成部分,为可能支持改进的Clp蛋白酶抑制剂的开发提供了见解。