Department of Chemistry and Chemical Biology, Harvard University, 12 Oxford Street, Cambridge, MA 02138, USA.
Bioorg Med Chem Lett. 2009 Nov 1;19(21):6189-91. doi: 10.1016/j.bmcl.2009.09.001. Epub 2009 Sep 6.
Ramoplanin is a potent lipoglycodepsipeptide antibiotic that is active against a wide range of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococcus (VRE). It acts as an inhibitor of peptidoglycan (PG) biosynthesis that disrupts glycan chain polymerization by binding and sequestering Lipid II, a PG precursor. Herein, we report the functional antimicrobial activity (MIC, S. aureus) and fundamental biochemical assessments against a peptidoglycan glycosyltransferase (Escherichia coli PBP1b) of a set of key alanine scan analogues of ramoplanin that provide insight into the importance and role of each of its individual amino acid residues.
雷莫拉宁是一种强效的脂糖肽类抗生素,对多种革兰氏阳性菌具有活性,包括耐甲氧西林金黄色葡萄球菌 (MRSA) 和耐万古霉素肠球菌 (VRE)。它作为肽聚糖 (PG) 生物合成的抑制剂,通过结合和隔离 PG 前体脂质 II 来破坏糖链聚合。在此,我们报告了一组雷莫拉宁关键丙氨酸扫描类似物的功能抗菌活性 (MIC、金黄色葡萄球菌) 和基本生化评估,这些评估提供了对其每个氨基酸残基的重要性和作用的深入了解。