Sch 34343的作用方式：对大肠杆菌K-12和脆弱拟杆菌青霉素结合蛋白的亲和力。

The mode of action of Sch 34343: affinity for the penicillin binding proteins of Escherichia coli K-12 and Bacteroides fragilis.

作者信息

Piddock L J, Wise R

出版信息

J Antimicrob Chemother. 1985 Jun;15 Suppl C:5-14. doi: 10.1093/jac/15.suppl_c.5.

DOI:10.1093/jac/15.suppl_c.5

Abstract

The competition of the new penem antibiotic, Sch 34343, for the penicillin-binding-proteins (PBPs) of Escherichia coli and Bacteroides fragilis was studied. Sch 34343 caused rounding of cells, and then sphaeroplast formation and lysis in both organisms. The primary target in both organisms was PBP 2, and at higher concentrations PBP 1a and 1b (and 1c in Bact. fragilis). These targets were inhibited at well below therapeutically achievable concentrations. The results indicate that in E. coli and Bact. fragilis, the bactericidal activity of Sch 34343 is related to inhibition of two out of three 'essential' PBPs.

摘要

研究了新型青霉烯抗生素Sch 34343对大肠杆菌和脆弱拟杆菌青霉素结合蛋白（PBPs）的竞争作用。Sch 34343可使两种菌的细胞变圆，随后形成原生质球并裂解。两种菌的主要靶点均为PBP 2，在较高浓度时为PBP 1a和1b（脆弱拟杆菌中为PBP 1c）。这些靶点在远低于治疗可达到的浓度时就受到抑制。结果表明，在大肠杆菌和脆弱拟杆菌中，Sch 34343的杀菌活性与抑制三种“必需”PBPs中的两种有关。