Echinocandins are the first class of antifungals to inhibit fungal cell wall biosynthesis.Anidulafungin and micafungin,two echinocandin derivatives are widely used in clinic,and are semisynthesized by replacements of the long chain fatty acyl side chains with artificial acyl side chains on the cyclic hexapeptide nuclei of echinocandin B (ECB) and FR901379,respectively.Aculeacin A acylase (AAC) and FR901379 acylases can catalyze the removal of the fatty acyl side chains from ECB and FR901379,generating ECB nucleus and FR901379 nucleus,respectively.AAC and FR901379 acylases have a strong acylase activity for echinocandins and can be heterologously overproduced in Streptomyces,making them green biocatalysts for the production of echinocandin medicines in pharmaceutical industry.Here we reviewed the characteristics and the applications of AAC and FR901379 acylases.%棘白霉素类化合物是最早发现的能抑制真菌细胞壁合成的天然产物,其中阿尼芬净和米卡芬净2种棘白霉素衍生物已经被广泛地应用于临床.它们的合成途径包括一个关键步骤,将天然产物棘白霉素B(ECB)和FR901379的6元环状多肽核上的长链脂肪酰侧链分别用非天然酰基侧链取代.阿库来菌素A酰基酶(AAC)和FR901379酰基酶能催化ECB和FR901379脂肪酰侧链的水解,生成的ECB和FR901379的环状多肽核可用于阿尼芬净和米卡芬净的生产.AAC和FR901379酰基酶对棘白霉素类化合物的酰基有很强的水解活性,而且这2个酶能在链霉菌中异源生产,因此它们成为棘白霉素类药物工业生产中广泛应用的绿色生物催化剂.本文介绍了ACC和FR901379酰基酶的酶学特性与应用.
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