Microbial and Plant Biotechnology Department, Centro de Investigaciones Biológicas Margarita Salas (CIB-CSIC), Madrid, Spain.
Department of Macromolecular Structure, Centro Nacional de Biotecnología (CNB-CSIC), Madrid, Spain.
Acta Crystallogr D Struct Biol. 2022 Apr 1;78(Pt 4):435-454. doi: 10.1107/S2059798322000936. Epub 2022 Mar 4.
Phage lysins are a source of novel antimicrobials to tackle the bacterial antibiotic-resistance crisis. The engineering of phage lysins is being explored as a game-changing technological strategy to introduce a more precise approach in the way in which antimicrobial therapy is applied. Such engineering efforts will benefit from a better understanding of lysin structure and function. In this work, the antimicrobial activity of the endolysin from Pseudomonas aeruginosa phage JG004, termed Pae87, has been characterized. This lysin had previously been identified as an antimicrobial agent candidate that is able to interact with the Gram-negative surface and disrupt it. Further evidence is provided here based on a structural and biochemical study. A high-resolution crystal structure of Pae87 complexed with a peptidoglycan fragment showed a separate substrate-binding region within the catalytic domain, 18 Å away from the catalytic site and located on the opposite side of the lysin molecule. This substrate-binding region was conserved among phylogenetically related lysins lacking an additional cell-wall-binding domain, but not among those containing such a module. Two glutamic acids were identified to be relevant for the peptidoglycan-degradation activity, although the antimicrobial activity of Pae87 was seemingly unrelated. In contrast, an antimicrobial peptide-like region within the Pae87 C-terminus, named P87, was found to be able to actively disturb the outer membrane and display antibacterial activity by itself. Therefore, an antimicrobial mechanism for Pae87 is proposed in which the P87 peptide plays the role of binding to the outer membrane and disrupting the cell-wall function, either with or without the participation of the catalytic activity of Pae87.
噬菌体裂解酶是解决细菌抗生素耐药性危机的新型抗菌药物的来源。噬菌体裂解酶的工程正在被探索作为一种改变游戏规则的技术策略,以引入更精确的抗菌治疗方法。这种工程努力将受益于对裂解酶结构和功能的更好理解。在这项工作中,已经对铜绿假单胞菌噬菌体 JG004 的内溶素,称为 Pae87 的抗菌活性进行了表征。该裂解酶先前被鉴定为一种能够与革兰氏阴性表面相互作用并破坏其结构的抗菌剂候选物。这里基于结构和生化研究提供了进一步的证据。Pae87 与肽聚糖片段复合物的高分辨率晶体结构显示,在催化结构域内有一个单独的底物结合区域,距离催化位点 18Å,位于裂解酶分子的对面。该底物结合区域在缺乏额外细胞壁结合结构域的系统发育相关裂解酶中是保守的,但在包含该模块的裂解酶中则不然。鉴定出两个谷氨酸对肽聚糖降解活性是相关的,尽管 Pae87 的抗菌活性似乎与之无关。相比之下,在 Pae87 C 末端发现的一个抗菌肽样区域,命名为 P87,能够主动扰乱外膜并独立显示抗菌活性。因此,提出了 Pae87 的抗菌机制,其中 P87 肽起到与外膜结合并破坏细胞壁功能的作用,无论是否有 Pae87 的催化活性参与。