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肺炎链球菌C型唾液酸酶的催化机制:从共价中间体到终产物

Catalytic mechanism of type C sialidase from Streptococcus pneumoniae: from covalent intermediate to final product.

作者信息

Xiong Jing, Zhang Chunchun, Xu Dingguo

机构信息

MOE Key Laboratory of Green Chemistry & Technology, College of Chemistry, Sichuan University, Chengdu, Sichuan, 610064, People's Republic of China.

School of Pharmacy, Chengdu Medical College, Chengdu, Sichuan, 610500, People's Republic of China.

出版信息

J Mol Model. 2018 Sep 26;24(10):297. doi: 10.1007/s00894-018-3822-5.

Abstract

Streptococcus pneumoniae is a Gram-positive human pathogenic bacterium, which is the main cause of pneumonia and meningitis in children and the elderly. Three sialidases (or neuraminidases) encoded from Streptococcus pneumoniae could catalyze the cleavage of sialic acid linkages. This mechanism is directly connected with infection, apoptosis, and signaling, and usually considered to be one of the critical virulence factors. Type C neuraminidase (NanC) is unique because its primary product of Neu5Ac2en is considered to be an inhibitor to the other two sialidases. Experimentally, there are two different pathways for the formation mechanism of Neu5Ac2en catalyzed by NanC. In this work, a combined quantum mechanical and molecular mechanical approach was employed in all calculations. Starting from the covalent sialylated intermediate, we first examined the reaction to Neu5Ac2en and found the reaction prefers a direct proton abstraction mechanism rather than the water mediated proton abstraction mechanism. Free energy profiles can confirm that Neu5Ac2en is the major product of NanC. Functional roles of some important residues were also investigated, e.g., D315 acts as the proton acceptor during the formation of Neu5Ac2en, while the general base for the hydrolytic reaction to Neu5Ac. This study can facilitate the understanding of the catalytic mechanism of NanC and has the potential to aid in future inhibitor design studies.

摘要

肺炎链球菌是一种革兰氏阳性人类致病细菌,是儿童和老年人肺炎及脑膜炎的主要病因。肺炎链球菌编码的三种唾液酸酶(或神经氨酸酶)可催化唾液酸键的裂解。这一机制与感染、细胞凋亡和信号传导直接相关,通常被认为是关键的毒力因子之一。C型神经氨酸酶(NanC)很独特,因为其主要产物Neu5Ac2en被认为是另外两种唾液酸酶的抑制剂。在实验中,NanC催化形成Neu5Ac2en的机制有两种不同途径。在这项工作中,所有计算均采用量子力学和分子力学相结合的方法。从共价唾液酸化中间体开始,我们首先研究了生成Neu5Ac2en的反应,发现该反应更倾向于直接质子提取机制而非水介导的质子提取机制。自由能剖面图可以证实Neu5Ac2en是NanC的主要产物。还研究了一些重要残基的功能作用,例如,D315在Neu5Ac2en形成过程中作为质子受体,而在对Neu5Ac水解反应中作为通用碱。这项研究有助于理解NanC的催化机制,并有可能为未来的抑制剂设计研究提供帮助。

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