Expression of two human acyl-CoA:diacylglycerol acyltransferase isozymes in yeast and selectivity of microbial inhibitors toward the isozymes.
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.
Inokoshi
Junji
J
School of Pharmacy, Kitasato University, Tokyo, Japan.
Kawamoto
Kyosuke
K
Takagi
Yoichi
Y
Matsuhama
Maki
M
Omura
Satoshi
S
Tomoda
Hiroshi
H
D000818:Animals; D018076:DNA, Complementary / Q000235:genetics; D051048:Diacylglycerol O-Acyltransferase / Q000037:antagonists & inhibitors* / Q000096:biosynthesis* / Q000235:genetics; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D008099:Liver / Q000201:enzymology; D008969:Molecular Sequence Data; D010957:Plasmids / Q000235:genetics; D051381:Rats; D020133:Reverse Transcriptase Polymerase Chain Reaction; D012441:Saccharomyces cerevisiae / Q000201:enzymology* / Q000235:genetics*
D018076:DNA, Complementary; D004791:Enzyme Inhibitors; D007527:Isoenzymes; C494881:DGAT1 protein, human; C494885:DGAT2 protein, human; D051048:Diacylglycerol O-Acyltransferase