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金黄色葡萄球菌PrsA的小菌素型肽脯氨酰顺反异构酶结构域的溶液结构——对小菌素催化机制的启示

Solution structure of the parvulin-type PPIase domain of Staphylococcus aureus PrsA--implications for the catalytic mechanism of parvulins.

作者信息

Heikkinen Outi, Seppala Raili, Tossavainen Helena, Heikkinen Sami, Koskela Harri, Permi Perttu, Kilpeläinen Ilkka

机构信息

Department of Chemistry, University of Helsinki, Finland.

出版信息

BMC Struct Biol. 2009 Mar 24;9:17. doi: 10.1186/1472-6807-9-17.

Abstract

BACKGROUND

Staphylococcus aureus is a Gram-positive pathogenic bacterium causing many kinds of infections from mild respiratory tract infections to life-threatening states as sepsis. Recent emergence of S. aureus strains resistant to numerous antibiotics has created a need for new antimicrobial agents and novel drug targets. S. aureus PrsA is a membrane associated extra-cytoplasmic lipoprotein which contains a parvulin-type peptidyl-prolyl cis-trans isomerase domain. PrsA is known to act as an essential folding factor for secreted proteins in Gram-positive bacteria and thus it is a potential target for antimicrobial drugs against S. aureus.

RESULTS

We have solved a high-resolution solution structure of the parvulin-type peptidyl-prolyl cis-trans isomerase domain of S. aureus PrsA (PrsA-PPIase). The results of substrate peptide titrations pinpoint the active site and demonstrate the substrate preference of the enzyme. With detailed NMR spectroscopic investigation of the orientation and tautomeric state of the active site histidines we are able to give further insight into the structure of the catalytic site. NMR relaxation analysis gives information on the dynamic behaviour of PrsA-PPIase.

CONCLUSION

Detailed structural description of the S. aureus PrsA-PPIase lays the foundation for structure-based design of enzyme inhibitors. The structure resembles hPin1-type parvulins both structurally and regarding substrate preference. Even though a wealth of structural data is available on parvulins, the catalytic mechanism has yet to be resolved. The structure of S. aureus PrsA-PPIase and our findings on the role of the conserved active site histidines help in designing further experiments to solve the detailed catalytic mechanism.

摘要

背景

金黄色葡萄球菌是一种革兰氏阳性病原菌,可引发多种感染,从轻度呼吸道感染到如败血症等危及生命的状态。最近出现的对多种抗生素耐药的金黄色葡萄球菌菌株使得需要新的抗菌剂和新型药物靶点。金黄色葡萄球菌PrsA是一种与膜相关的胞外脂蛋白,其含有一个小菌素型肽基脯氨酰顺反异构酶结构域。已知PrsA在革兰氏阳性细菌中作为分泌蛋白的必需折叠因子发挥作用,因此它是针对金黄色葡萄球菌的抗菌药物的潜在靶点。

结果

我们解析了金黄色葡萄球菌PrsA的小菌素型肽基脯氨酰顺反异构酶结构域(PrsA-PPIase)的高分辨率溶液结构。底物肽滴定结果确定了活性位点并证明了该酶的底物偏好性。通过对活性位点组氨酸的取向和互变异构状态进行详细的核磁共振光谱研究,我们能够进一步深入了解催化位点的结构。核磁共振弛豫分析给出了PrsA-PPIase动态行为的信息。

结论

对金黄色葡萄球菌PrsA-PPIase的详细结构描述为基于结构的酶抑制剂设计奠定了基础。该结构在结构和底物偏好方面都类似于hPin1型小菌素。尽管关于小菌素已有大量结构数据,但催化机制尚未得到解析。金黄色葡萄球菌PrsA-PPIase的结构以及我们关于保守活性位点组氨酸作用的发现有助于设计进一步的实验来解析详细的催化机制。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e3a/2678132/9c54479fd606/1472-6807-9-17-1.jpg

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