半合成糖肽类抗生素达巴万星前体A40926的生物合成

Biosynthesis of A40926,A Precursor of Semisynthesis Glycopeptide Antibiotic Dalbavancin

综述了继替考拉宁之后的第二代半合成糖肽类抗生素达巴万星前体A40926的研究进展,包括其结构、发酵生产、生物合成以及结构修饰。重点阐述了A40926的生物合成基因簇以及合成途径。达巴万星是A40926的半合成化合物,目前处于Ⅲ期临床研究,它具有比万古霉素和替考拉宁更强的生物活性。

It was reviewed that the recent advance on A40926, a precursor of a second-generation glycopeptides antibiotic, dalbavancin, developed after teicoplanin, including the structure, fermentation production, biosynthesis and structural modification of A40926. The biosynthesis gene clusters and synthetic route of A40926 were especially introduced. Dalbavancin, a novel semisynthetic derivative of A40926, showing more potent than vancomycin and teicoplanin, is now in the phase III clinical trials.