昆虫几丁质合成酶及其抑制剂

Chitin synthase from insects and its inhibitors

几丁质合成酶(CS)是几丁质合成的关键酶,它具有3个结构域:结构域A、结构域B和结构域C,其中结构域B是催化域。根据氨基酸序列的差异,几丁质合成酶分为两类:CS-A及CS-B,分别在表皮及围食膜基质中催化合成几丁质。关于几丁质合成有2种假想模型。有多种抑制剂可以抑制几丁质的合成,其中核苷肽抗生素类及核苷磷酸类作用于CS的催化部位,是竞争性抑制剂,其它抑制剂的作用机理仍不明确。

Chitin synthase is the key enzyme in the synthesis of chitin, which has three domains ： domain A, domain B and domain C; domain B is the catalytic center. Based on relative sequence differences, chitin synthases have been grouped into two classes, class CS-A and class CS-B enzymes, which catalyze the formation of chitin in epidermis and peritrophic matrix respectively. Two model of catalyze mechanism was suggested. There are many chemicals that can inhibit the synthesis of chitin, of which nucleoside peptidyl antibiotics and nucleoside phosphates are acting on the catalytic site of CS as competitive inhibitors; however, other chemicals＇ inhibition mode is still unknown.