Diacylglycerol O-Acyltransferase

Diacylglycerol O-Acyltransferases (DGATs), EC 2.3.1.20, are enzymes that catalyze the final step of triglyceride (TG) synthesis, the covalent attachment of fatty acyl-CoA and diacylglycerol (DAG). There have been two DGAT isoforms identified to date, DGAT1 and DGAT2.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
3587 A 922500
Potent DGAT-1 inhibitor
4837 AZD 3988
Potent and selective DGAT-1 inhibitor
5853 JNJ DGAT2-A
DGAT2 inhibitor
5863 PF 04620110
Potent and selective DGAT-1 inhibitor; orally bioavailable
4686 Xanthohumol
Diacylglycerol acyltransferase (DGAT) inhibitor

Diacylglycerol O-Acyltransferases (DGATs), EC 2.3.1.20, are enzymes that catalyze the final step of triglyceride (TG) synthesis, the covalent attachment of fatty acyl-CoA and diacylglycerol (DAG). There have been two DGAT isoforms identified to date, DGAT1 and DGAT2, which are members of the MBOAT and DAGAT families of acyltransferases, respectively.

DGAT1/2 have a wide expression profile, being highly expressed in adipocytes, hepatocytes, enterocytes and the mammary gland, and are typically found in the endoplasmic reticulum, the site of TG synthesis. Expression of DGAT1/2 can be regulated by adipogenesis, as well as glucose and insulin levels. PPARγ and C/EBPα are thought to upregulate DGAT1/2 mRNA expression, whereas MEK-ERK signaling may suppress gene expression.

DGATs play a role in energy and glucose metabolism, as well as tissue development. Obesity is associated with an excessive accumulation of TG and DGAT inhibition has been shown to reduce weight gain in diet-induced obese mice. DGAT1 deficiency also enhances glucose metabolism in mice, while inhibition of hepatic DGAT2 has been shown to decrease insulin resistance in mice fed a high-fat diet. Consequently the DGAT isoforms are potential therapeutic targets for the treatment of obesity and diabetes.

External sources of pharmacological information for Diacylglycerol O-Acyltransferase :

    Literature for Diacylglycerol O-Acyltransferase

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    Diacylglycerol O-Acyltransferase Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    DGAT1 Human DGAT1 NM_012079 O75907
    Mouse Dgat1 NM_010046 Q9Z2A7
    Rat Dgat1 NM_053437 Q9ERM3
    DGAT2 Human DGAT2 NM_032564 Q96PD7
    Mouse Dgat2 NM_026384 Q9DCV3
    Rat Dgat2 NM_001012345 Q5FVP8