Röhl F, Rabenhorst J, Zähner H
Arch Microbiol. 1987 May;147(4):315-20. doi: 10.1007/BF00406126.
The clavams valclavam and hydroxyethylclavam were both bacteriostatic and fungistatic. The molecular basis for growth inhibition of Escherichia coli was a non-competitive inhibition of homoserine-O-succinyltransferase (EC 2.3.1.46), thus blocking methionine biosynthesis. Eucaryotes such as Saccharomyces cerevisiae were inhibited by a different mode of action. Instead of interfering with methionine biosynthesis, the clavams inhibited the formation of RNA in living cells, although the RNA-polymerases of isolated yeast nuclei were not inhibited. The action of valclavam on E. coli was dependent on functional peptide transport systems.
棒酸衍生物瓦克拉维酸和羟乙基棒酸均具有抑菌和抑真菌作用。抑制大肠杆菌生长的分子基础是对高丝氨酸 - O - 琥珀酰转移酶(EC 2.3.1.46)的非竞争性抑制,从而阻断甲硫氨酸的生物合成。酿酒酵母等真核生物受到的抑制作用方式不同。棒酸衍生物不是干扰甲硫氨酸的生物合成,而是抑制活细胞中RNA的形成,尽管分离的酵母细胞核的RNA聚合酶未受抑制。瓦克拉维酸对大肠杆菌的作用依赖于功能性肽转运系统。