State Key Laboratory of Microbial Metabolism, Joint International Research Laboratory of Metabolic and Developmental Sciences, School of Life Sciences and Biotechnology, Shanghai Jiao Tong University, Shanghai 200240, China.
Kobilka Institute of Innovative Drug Discovery, School of Life and Health Sciences, The Chinese University of Hong Kong, Shenzhen 518172, China.
Proc Natl Acad Sci U S A. 2021 Jul 27;118(30). doi: 10.1073/pnas.2102318118.
Blasticidin S is a peptidyl nucleoside antibiotic. Its biosynthesis involves a cryptic leucylation and two leucylated intermediates, LDBS and LBS, have been found in previous studies. Leucylation has been proposed to be a new self-resistance mechanism during blasticidin S biosynthesis, and the leucyl group was found to be important for the methylation of β-amino group of the arginine side chain. However, the responsible enzyme and its associated mechanism of the leucyl transfer process remain to be elucidated. Here, we report results investigating the leucyl transfer step forming the intermediate LDBS in blasticidin biosynthesis. A hypothetical protein, BlsK, has been characterized by genetic and in vitro biochemical experiments. This enzyme catalyzes the leucyl transfer from leucyl-transfer RNA (leucyl-tRNA) to the β-amino group on the arginine side chain of DBS. Furthermore, BlsK was found to contain an iron-sulfur cluster that is necessary for activity. These findings provide an example of an iron-sulfur protein that catalyzes an aminoacyl-tRNA (aa-tRNA)-dependent amide bond formation in a natural product biosynthetic pathway.
硫酸博莱霉素 S 是一种肽核苷抗生素。其生物合成涉及一个隐匿的亮氨酰化作用,并且在先前的研究中发现了两种亮氨酰化中间产物 LDBS 和 LBS。亮氨酰化被提议为硫酸博莱霉素生物合成过程中的一种新的自我抗性机制,并且亮氨酰基对于精氨酸侧链的β-氨基的甲基化是重要的。然而,负责的酶及其相关的亮氨酰转移过程的机制仍有待阐明。在这里,我们报告了研究在硫酸博莱霉素生物合成中形成中间产物 LDBS 的亮氨酰转移步骤的结果。通过遗传和体外生化实验,鉴定了一个假定的蛋白 BlsK。该酶催化从亮氨酰-tRNA 到 DBS 的精氨酸侧链的β-氨基上的亮氨酰基转移。此外,发现 BlsK 含有一个对于活性是必需的铁硫簇。这些发现提供了一个铁硫蛋白的例子,该蛋白在天然产物生物合成途径中催化依赖于氨酰-tRNA(aa-tRNA)的酰胺键形成。