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米卡芬净:一种硫酸化棘白菌素。

Micafungin: a sulfated echinocandin.

作者信息

Hashimoto Seiji

机构信息

Biotechnology Research Center, Faculty of Engineering, Toyama Prefectural University, Imizu, Toyama, Japan.

出版信息

J Antibiot (Tokyo). 2009 Jan;62(1):27-35. doi: 10.1038/ja.2008.3. Epub 2009 Jan 9.

Abstract

Micafungin is the second approved antifungal agent in the echinocandin series and is now used worldwide in chemotherapy for life-threatening fungal infections. It is water-soluble and is semi-synthesized from the acylated cyclic hexapeptide FR901379, a natural product from the fungus Coleophoma empetri F-11899, through enzymatic deacylation of FR901379, followed by chemical reacylation with the optimized N-acyl side chain. The water solubility of micafungin is ascribed to a sulfate moiety in the molecule. This feature differentiates micafungin from other echinocandin members. Micafungin is a potent inhibitor of 1,3-beta-glucan synthase, an enzyme necessary for cell-wall synthesis of several fungal pathogens.

摘要

米卡芬净是棘白菌素系列中第二个获批的抗真菌药物,目前在全球范围内用于治疗危及生命的真菌感染的化疗。它是水溶性的,由酰化环六肽FR901379(一种来自真菌科尔皮菌F-11899的天然产物)经酶促脱酰基作用,然后与优化的N-酰基侧链进行化学再酰化反应半合成得到。米卡芬净的水溶性归因于分子中的硫酸根部分。这一特性使米卡芬净有别于其他棘白菌素成员。米卡芬净是1,3-β-葡聚糖合酶的强效抑制剂,该酶是几种真菌病原体细胞壁合成所必需的。

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