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两种人类酰基辅酶A:二酰基甘油酰基转移酶同工酶在酵母中的表达以及微生物抑制剂对这些同工酶的选择性。

Expression of two human acyl-CoA:diacylglycerol acyltransferase isozymes in yeast and selectivity of microbial inhibitors toward the isozymes.

作者信息

Inokoshi Junji, Kawamoto Kyosuke, Takagi Yoichi, Matsuhama Maki, Omura Satoshi, Tomoda Hiroshi

机构信息

School of Pharmacy, Kitasato University, Tokyo, Japan.

出版信息

J Antibiot (Tokyo). 2009 Jan;62(1):51-4. doi: 10.1038/ja.2008.5. Epub 2009 Jan 9.

Abstract

Two isozymes for human acyl-coenzyme A:diacylglycerol acyltransferase (DGAT), DGAT1 and DGAT2, were independently expressed in DGAT-deficient Saccharomyces cerevisiae to establish DGAT1- and DGAT2-S. cerevisiae. The selectivity of DGAT inhibitors of natural origin towards the isozymes was assessed in enzyme assays using the microsomal fractions prepared from DGAT1- and DGAT2-S. cerevisiae. Amidepsines and xanthohumol inhibited DGAT1 and DGAT2 with similar potency, whereas roselipins were found to inhibit DGAT2 selectively.

摘要

人类酰基辅酶A:二酰甘油酰基转移酶(DGAT)的两种同工酶DGAT1和DGAT2在缺乏DGAT的酿酒酵母中独立表达,从而构建了DGAT1 - 酿酒酵母和DGAT2 - 酿酒酵母。使用从DGAT1 - 酿酒酵母和DGAT2 - 酿酒酵母制备的微粒体组分,通过酶测定评估了天然来源的DGAT抑制剂对这些同工酶的选择性。酰胺菌素和黄腐酚对DGAT1和DGAT2的抑制效力相似,而玫瑰脂素被发现可选择性抑制DGAT2。

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