昆虫I家族N-乙酰-D-己糖胺酶的结构、功能与抑制剂

Insect family I N-acetyl-D-hexosaminidase: structure, function and inhibitors

昆虫I家族N-乙酰-D-己糖胺酶Hex1(N-acetyl-D-hexosaminidase family I)是昆虫蜕皮和变态发育中不可或缺的几丁质水解酶.下调或干扰Hex1基因表达水平将导致昆虫蜕皮不正常而死亡.Hex1在生理功能上是特异的表皮几丁质降解酶,功能区别于人类以及高等动植物的同源酶,因此,Hex1可能成为潜在的农药创制靶标.近10年来,昆虫Hex1的研究在生物学和化学生物学等领域取得了突出进展.其中,来源于农业害虫亚洲玉米螟—Hex1(OfHex1)的晶体结构的解析取得重要进展,为针对Hex1的农用小分子理性设计提供理论基础.本文重点针对OfHex1的生理功能、结构特征以及选择性抑制剂等方面的研究进展进行综述.

Insect family I N-acetyl-D-hexosaminidase Hex1 is an indispensable chitinolytic enzyme for molting and metamorphosis. Down-regulation or interference of Hex1 gene expression causes abnormality of molting and then lethality. Since Hex1 is a specialized chitin degradation enzyme different from its homologs that from plants and high-class animals, Hex1 is considered to be a promising green agro-target. Research progress of Hex1 in the last decade was exciting, in particular the crystal structure resolution of Of Hex1, the Hex1 from a serious crop pest, Asian corn borer. The crystal structure of Of Hex1 first provides detailed basis of developing agrochemicals. This review focuses on recent progress on Of Hex1, including physiological importance, structural characteristics as well as selective inhibitors.