革兰阴性菌LpxC抑制剂的研究进展

Research progress of LpxC inhibitor on Gram-negative bacteria

UDP-3-O-(R-羟基十四酰)-N-乙酰氨基葡糖脱乙酰酶(脱乙酰酶)为一种金属酶(辅助因子为锌),是催化革兰阴性菌外膜脂多糖主要成分类脂A合成的关键酶,且与哺乳动物的各种酶蛋白都没有共同氨基酸序列。LpxC是革兰阴性菌存活的必需酶,目前已经发现该酶可以作为抗菌药物的靶点。本文对LpxC的结构、酶催化机理及其新型抑制剂的研究进展进行综述。

UDP-3-O-acyl-N-acetylglucosamine deacetylase(LpxC)is a metal enzyme with the cofactor of zinc.It is a key enzyme that catalyzes the synthesis of major component Lipid A of Gram-negative bacteria outer membrane lipopolysaccharide,and has no common amino acid sequence with various mammalian enzyme proteins.LpxC is an essential enzyme for the survival of Gram-negative bacteria,and it has been found that LpxC can be used as a target for antibacterial drugs.This paper reviews the research progress on the structure of LpxC,mechanism of enzymatic catalysis and new inhibitors.