Inokoshi Junji, Kawamoto Kyosuke, Takagi Yoichi, Matsuhama Maki, Omura Satoshi, Tomoda Hiroshi
School of Pharmacy, Kitasato University, Tokyo, Japan.
J Antibiot (Tokyo). 2009 Jan;62(1):51-4. doi: 10.1038/ja.2008.5. Epub 2009 Jan 9.
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.
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。