Russell Rupert J M, Murray James B, Lentzen Georg, Haddad Jalal, Mobashery Shahriar
RiboTargets, Granta Park, Cambridge CB1 6GB, United Kingdom.
J Am Chem Soc. 2003 Mar 26;125(12):3410-1. doi: 10.1021/ja029736h.
The ribosome is an important target for aminoglycoside antibiotics; however, the clinical effectiveness of aminoglycosides has diminished due to bacterial resistance mechanisms. Here we report the X-ray structure of a novel synthetic aminoglycoside bound to the A site of the ribosome, its target for manifestation of activity. The structure validates the in silico design paradigms for the antibiotic and reveals the molecular interactions made by this novel antibiotic in prokaryotes.
核糖体是氨基糖苷类抗生素的重要靶点；然而，由于细菌耐药机制，氨基糖苷类药物的临床疗效已经降低。在此，我们报告了一种新型合成氨基糖苷与核糖体A位点结合的X射线结构，A位点是其发挥活性的靶点。该结构验证了该抗生素的计算机辅助设计模式，并揭示了这种新型抗生素在原核生物中的分子相互作用。
