Liu Xiaodong, Jin Yuanyuan, Cui Zheng, Nonaka Koichi, Baba Satoshi, Funabashi Masanori, Yang Zhaoyong, Van Lanen Steven G
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY, 40536, USA.
Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medicinal Sciences & Peking Union Medical College, Beijing, China.
Chembiochem. 2016 May 3;17(9):804-10. doi: 10.1002/cbic.201500701. Epub 2016 Mar 18.
Capuramycins are one of several known classes of natural products that contain an l-Lys-derived l-α-amino-ɛ-caprolactam (l-ACL) unit. The α-amino group of l-ACL in a capuramycin is linked to an unsaturated hexuronic acid component through an amide bond that was previously shown to originate by an ATP-independent enzymatic route. With the aid of a combined in vivo and in vitro approach, a predicted tridomain nonribosomal peptide synthetase CapU is functionally characterized here as the ATP-dependent amide-bond-forming catalyst responsible for the biosynthesis of the remaining amide bond present in l-ACL. The results are consistent with the adenylation domain of CapU as the essential catalytic component for l-Lys activation and thioesterification of the adjacent thiolation domain. However, in contrast to expectations, lactamization does not require any additional domains or proteins and is likely a nonenzymatic event. The results set the stage for examining whether a similar NRPS-mediated mechanism is employed in the biosynthesis of other l-ACL-containing natural products and, just as intriguingly, how spontaneous lactamization is avoided in the numerous NRPS-derived peptides that contain an unmodified l-Lys residue.
卡普霉素是几种已知的天然产物类别之一,这些天然产物含有一个源自L-赖氨酸的L-α-氨基-ε-己内酰胺(L-ACL)单元。卡普霉素中L-ACL的α-氨基通过一个酰胺键与一个不饱和己糖醛酸成分相连,此前已证明该酰胺键是通过一条不依赖ATP的酶促途径形成的。借助体内和体外相结合的方法,预测的三结构域非核糖体肽合成酶CapU在此被功能表征为负责L-ACL中剩余酰胺键生物合成的依赖ATP的酰胺键形成催化剂。结果表明CapU的腺苷化结构域是L-赖氨酸激活和相邻硫醇化结构域硫酯化的关键催化成分。然而,与预期相反,内酰胺化不需要任何额外的结构域或蛋白质,可能是一个非酶促事件。这些结果为研究其他含L-ACL的天然产物的生物合成中是否采用类似的NRPS介导机制奠定了基础,同样有趣的是,在众多含有未修饰L-赖氨酸残基的NRPS衍生肽中,如何避免自发内酰胺化。