【摘要】 细菌的耐药性问题日益严峻,给临床治疗带来极大困难。研发新型抗耐药菌药物,寻找新的靶点成为目前的研究热点。肽脱甲酰基酶(peptide deformylase,PDF)是细菌蛋白质合成过程中的一种关键酶,普遍存在于大多数病原体中,且易于进行体外检测,是一个较理想的靶点。本文简单介绍了PDF的结构、催化机制,系统归纳了近年来PDF抑制剂结构修饰及构效关系方面的研究进展。构效关系研究表明具有较强抑制作用的PDF抑制剂多为拟肽类化合物。在PDF抑制剂的筛选中,其选择性应得到重视。更多还原

【Abstract】 Currently,the emergence of the drug-resistance bacteria brings lots of difficulties to clinical treatment.Therefore,identification of new targets and development of new drug with a low resistance profile and high potency remains the subject of intensive research.Peptide deformylase(PDF)is an essential enzyme that involves prorein biosynthesis of bacteria,which is found in all prokaryocytes,and also considered to be one of the most promising target leading to a new generation of broad-spectrum antibiotics.This article reviews the structure and catalytic mechanism of PDF.The recent progress in the structural modification and structure-activity relationship of PDF inhibitors are addressed.The structure-activity relationship illuminates that PDF inhibitors with high activity are pseudopeptide compounds, and its selection should be emphasized in the biological evaluation.更多还原