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Literature summary for 2.3.1.20 extracted from

  • Wurie, H.R.; Buckett, L.; Zammit, V.A.
    Diacylglycerol acyltransferase 2 acts upstream of diacylglycerol acyltransferase 1 and utilizes nascent diglycerides and de novo synthesized fatty acids in HepG2 cells (2012), FEBS J., 279, 3033-3047.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in baculoviral system Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
N-(4,5-dihydronaphtho[1,2-d]thiazol-2-yl)-2-(3,4-dimethoxy phenyl)acetamide selective inhibitor of isoform DGAT2 when used at low concentrations; selective inhibitor of isoform DGAT2 when used at low concentrations Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O75907 isoform DGAT1
-
Homo sapiens Q96PD7 isoform DGAT2
-

Source Tissue

Source Tissue Comment Organism Textmining
Hep-G2 cell
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
DGAT1
-
Homo sapiens
DGAT2
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0085
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-(4,5-dihydronaphtho[1,2-d]thiazol-2-yl)-2-(3,4-dimethoxy phenyl)acetamide
0.0708
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-(4,5-dihydronaphtho[1,2-d]thiazol-2-yl)-2-(3,4-dimethoxy phenyl)acetamide

General Information

General Information Comment Organism
physiological function inhibition of isoform DGAT1 affects equally the incorporation of glycerol and exogenous preformed oleate into cellular and secreted triacylglycerol. Data indicate that isoform DGAT2 acts upstream of isoform DGAT1, and DGAT1 functions in the re-esterification of partial glycerides generated by intracellular lipolysis, using preformed fatty acids Homo sapiens
physiological function isoform DGAT2 activity accounts for a modest fraction of less than 20% of overall cellular DGAT activity. Inhibition of DGAT2 activity specifically inhibits and is rate-limiting for the incorporation of de novo synthesized fatty acids and of glycerol into cellular and secreted triglyceride to a much greater extent than it affects the incorporation of exogenously added oleate. Isoform DGAT2 acts upstream of isoform DGAT1, largely determines the rate of de novo synthesis of triglyceride, and uses nascent diacylglycerol and de novo synthesized fatty acids as substrates Homo sapiens