Phenylacetyl pepstatin inhibitors of aspartyl proteases from Streptomyces varsoviensis,The Journal of Antibiotics

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Phenylacetyl pepstatin inhibitors of aspartyl proteases from Streptomyces varsoviensis
The Journal of Antibiotics ( IF 2.1 ) Pub Date : 2022-07-26 , DOI: 10.1038/s41429-022-00542-6
Weijian Ye ₁ , Zhihong Guo ₁

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A new pepstatin with a phenylacetyl group, pepstatin Pa (1), and its methyl ester (2) were isolated from Streptomyces varsoviensis DSM 40346. Their structures were determined by high-resolution mass spectrometry and nuclear magnetic resonance techniques. The absolute configuration was determined using the Marfey’s method. Both pentapeptide products are inhibitors of pepsin and cathepsin D. Interestingly, the bacterial genome contains no biosynthetic gene cluster for the new pepstatin, suggesting an extrachromosomal origin of the biosynthetic genes.

中文翻译：

来自 Streptomyces varsoviensis 的天冬氨酰蛋白酶的苯乙酰胃酶抑素抑制剂

从Streptomyces varsoviensis DSM 40346中分离出一种带有苯乙酰基的新型胃酶抑素，胃酶抑素 Pa ( 1 ) 及其甲酯 ( 2 )。它们的结构通过高分辨率质谱和核磁共振技术确定。绝对配置是使用 Marfey 方法确定的。两种五肽产物都是胃蛋白酶和组织蛋白酶 D 的抑制剂。有趣的是，细菌基因组不包含新胃酶抑素的生物合成基因簇，表明生物合成基因起源于染色体外。

更新日期：2022-07-26

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