Brown Murray J, Carter Paul S, Fenwick Ashley S, Fosberry Andrew P, Hamprecht Dieter W, Hibbs Martin J, Jarvest Richard L, Mensah Lucy, Milner Peter H, O'Hanlon Peter J, Pope Andrew J, Richardson Christine M, West Andrew, Witty David R
GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.
Bioorg Med Chem Lett. 2002 Nov 4;12(21):3171-4. doi: 10.1016/s0960-894x(02)00604-2.
The antimicrobial natural product chuangxinmycin has been found to be a potent and selective inhibitor of bacterial tryptophanyl tRNA synthetase (WRS). A number of analogues have been synthesised. The interaction with WRS appears to be highly constrained, as only sterically smaller analogues afforded significant inhibition. The only analogue to show inhibition comparable to chuangxinmycin also had antibacterial activity. WRS inhibition may contribute to the antibacterial action of chuangxinmycin.
抗菌天然产物创新霉素已被发现是细菌色氨酰-tRNA合成酶（WRS）的一种强效且选择性抑制剂。已经合成了许多类似物。与WRS的相互作用似乎受到高度限制，因为只有空间上较小的类似物才有显著抑制作用。唯一显示出与创新霉素相当抑制作用的类似物也具有抗菌活性。WRS抑制可能有助于创新霉素的抗菌作用。
