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结构洞察甲壳素酶和选择性抑制剂的抑制机制。

Structural insights into chitinolytic enzymes and inhibition mechanisms of selective inhibitors.

机构信息

Linggong Road, Dalian 116024, China.

出版信息

Curr Pharm Des. 2014;20(5):754-70. doi: 10.2174/138161282005140214164730.

DOI:10.2174/138161282005140214164730
PMID:23688083
Abstract

Chitin biodegradation is linked to fungi cell differentiation, nematode egg hatching, arthropods morphogenesis and human defense against malaria and other pathogens infection as well. Two classes of enzymes for chitin degradation include glycosyl hydrolase (GH) family 18 chitinases and family 20 β-N-acetyl-D-hexosaminidases. However, more and more research papers have revealed that either GH 18 family chitinases or GH 20 family β-N-acetyl-D-hexosaminidases are a family composed of a number of isoforms, each of which plays an exclusive role in different life processes. The development of novel and specific inhibitors towards chitinolytic enzymes is of great importance in the investigation of or interference with chitin biodegradation. This review focuses on identified enzymes that are specifically involved in chitin degradation. And the latest progresses on crystal structures and specific inhibitors are summarized within the realm of this field.

摘要

几丁质生物降解与真菌细胞分化、线虫卵孵化、节肢动物形态发生以及人类抵抗疟疾和其他病原体感染有关。参与几丁质降解的两类酶包括糖苷水解酶(GH)家族 18 几丁质酶和家族 20β-N-乙酰-D-氨基葡萄糖苷酶。然而,越来越多的研究论文表明,GH 18 家族几丁质酶或 GH 20 家族β-N-乙酰-D-氨基葡萄糖苷酶是由许多同工酶组成的家族,每个同工酶在不同的生命过程中发挥独特的作用。新型和特异性几丁质酶抑制剂的开发对于研究或干扰几丁质生物降解具有重要意义。本综述重点介绍了特异性参与几丁质降解的酶。并总结了该领域内晶体结构和特异性抑制剂的最新进展。

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