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monoacylglycerol O-acyltransferase 2

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Target not currently curated in GtoImmuPdb

Target id: 2881

Nomenclature: monoacylglycerol O-acyltransferase 2

Family: 2.3.1.- Acyltransferases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 3 334 11q13.5 MOGAT2 monoacylglycerol O-acyltransferase 2 3
Mouse 2 334 7 E1 Mogat2 monoacylglycerol O-acyltransferase 2 2
Rat - 334 1q32 Mogat2 monoacylglycerol O-acyltransferase 2
Previous and Unofficial Names Click here for help
DGAT2L5 | MGAT2
Database Links Click here for help
Alphafold Q3SYC2 (Hs), Q80W94 (Mm)
BRENDA 2.3.1.22
ChEMBL Target CHEMBL2439944 (Hs), CHEMBL3603729 (Mm)
Ensembl Gene ENSG00000166391 (Hs), ENSMUSG00000052396 (Mm), ENSRNOG00000027228 (Rn)
Entrez Gene 80168 (Hs), 233549 (Mm), 681211 (Rn)
Human Protein Atlas ENSG00000166391 (Hs)
KEGG Enzyme 2.3.1.22
KEGG Gene hsa:80168 (Hs), mmu:233549 (Mm), rno:681211 (Rn)
OMIM 610270 (Hs)
Pharos Q3SYC2 (Hs)
RefSeq Nucleotide NM_025098 (Hs), NM_177448 (Mm), NM_001109436 (Rn)
RefSeq Protein NP_079374 (Hs), NP_803231 (Mm), NP_001102906 (Rn)
UniProtKB Q3SYC2 (Hs), Q80W94 (Mm)
Wikipedia MOGAT2 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.3.1.22
Description Reaction Reference
Acyl-CoA + 2-acylglycerol <=> CoA + diacylglycerol 4

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
BMS-986172 Small molecule or natural product Hs Inhibition 8.3 pIC50 5
⤷ pIC50 8.3 (IC50 4.6x10-9 M) [5]
BMS-963272 Small molecule or natural product Hs Inhibition 8.1 pIC50 8
⤷ pIC50 8.1 (IC50 7.1x10-9 M) [8]
BMS-963272 Small molecule or natural product Mm Inhibition 7.7 pIC50 8
⤷ pIC50 7.7 (IC50 1.8x10-8 M) [8]
BMS-986172 Small molecule or natural product Mm Inhibition 7.7 pIC50 5
⤷ pIC50 7.7 (IC50 2x10-8 M) [5]
View species-specific inhibitor tables
Tissue Distribution Click here for help
Intestine and liver
Species:  Human
Technique:  Northern blot
References:  3
Physiological Consequences of Altering Gene Expression Click here for help
Mogat2 deficient mice are protected from diet-induced obesity and glucose intolerance.
Species:  Mouse
Tissue: 
Technique:  Gene knockout and inducible Mogat2-inactivating mutation.
References:  1
General Comments
Results from genetic studies in mice [1,6-7] suggest that pharmacoligical inhibition of MOGAT2 may be a useful strategy for controlling metabolic disorders induced by high-fat diet.

References

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1. Banh T, Nelson DW, Gao Y, Huang TN, Yen MI, Yen CL. (2015) Adult-onset deficiency of acyl CoA:monoacylglycerol acyltransferase 2 protects mice from diet-induced obesity and glucose intolerance. J Lipid Res, 56 (2): 379-89. [PMID:25535286]

2. Cao J, Lockwood J, Burn P, Shi Y. (2003) Cloning and functional characterization of a mouse intestinal acyl-CoA:monoacylglycerol acyltransferase, MGAT2. J Biol Chem, 278 (16): 13860-6. [PMID:12576479]

3. Lockwood JF, Cao J, Burn P, Shi Y. (2003) Human intestinal monoacylglycerol acyltransferase: differential features in tissue expression and activity. Am J Physiol Endocrinol Metab, 285 (5): E927-37. [PMID:12824082]

4. Manganaro F, Kuksis A. (1985) Purification and preliminary characterization of 2-monoacylglycerol acyltransferase from rat intestinal villus cells. Can J Biochem Cell Biol, 63 (5): 341-7. [PMID:4016575]

5. Meng W, Brigance R, Mignone J, Negash L, Zhao G, Ahmad S, Wang W, Moore F, Ye XY, Sun JH et al.. (2023) Discovery of 12 (BMS-986172) as a Highly Potent MGAT2 Inhibitor that Achieved Targeted Efficacious Exposures at a Low Human Dose for the Treatment of Metabolic Disorders. J Med Chem, 66 (18): 13135-13147. [PMID:37724542]

6. Nelson DW, Gao Y, Spencer NM, Banh T, Yen CL. (2011) Deficiency of MGAT2 increases energy expenditure without high-fat feeding and protects genetically obese mice from excessive weight gain. J Lipid Res, 52 (9): 1723-32. [PMID:21734185]

7. Nelson DW, Gao Y, Yen MI, Yen CL. (2014) Intestine-specific deletion of acyl-CoA:monoacylglycerol acyltransferase (MGAT) 2 protects mice from diet-induced obesity and glucose intolerance. J Biol Chem, 289 (25): 17338-49. [PMID:24784138]

8. Turdi H, Chao H, Hangeland JJ, Ahmad S, Meng W, Brigance R, Zhao G, Wang W, Moore F, Ye XY et al.. (2021) Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders. J Med Chem, 64 (19): 14773-14792. [PMID:34613725]

How to cite this page

2.3.1.- Acyltransferases: monoacylglycerol O-acyltransferase 2. Last modified on 23/10/2023. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2881.