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Information on EC 2.3.1.22 - 2-acylglycerol O-acyltransferase and Organism(s) Homo sapiens and UniProt Accession Q96PD6
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2.3.1.22 2-acylglycerol O-acyltransferaseIUBMB Comments
Various 2-acylglycerols can act as acceptor; palmitoyl-CoA and other long-chain acyl-CoAs can act as donors. The sn-1 position and the sn-3 position are both acylated, at about the same rate.
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Word Map
- 2.3.1.22
- n-glycans
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mgats
- diacylglycerols
- triacylglycerol
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n-acetylglucosaminyltransferase
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bisect
- glcnac
- gnt-iii
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nipecotic
-
glycome
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tiagabine
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acyl-coa:diacylglycerol
- medicine
- st6gal1
- drug development
- pharmacology
- analysis
The taxonomic range for the selected organisms is: Homo sapiens
The expected taxonomic range for this enzyme is: Bacteria, Eukaryota
The expected taxonomic range for this enzyme is: Bacteria, Eukaryota
Synonyms
mgat1, mgat2, mgat3, mogat1, lpgat1, mogat2, mogat3, acyl-coa:monoacylglycerol acyltransferase, monoacylglycerol o-acyltransferase, monoacylglycerol o-acyltransferase 1, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
acyl coenzyme A-monoglyceride acyltransferase
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acyl-CoA:monoacylglycerol transferase
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acylglycerol palmitoyltransferase
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MGAT
monoacylglycerol acyltransferase
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monoglyceride acyltransferase
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palmitoyltransferase, acylglycerol
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additional information
MGAT
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additional information
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the enzyme belongs to the acyl-CoA:diacylglycerol acyltransferase 2/acyl-CoA:monoacylglycerol acyltransferase, MGAT, gene family
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Acyl group transfer
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SYSTEMATIC NAME
IUBMB Comments
acyl-CoA:2-acylglycerol O-acyltransferase
Various 2-acylglycerols can act as acceptor; palmitoyl-CoA and other long-chain acyl-CoAs can act as donors. The sn-1 position and the sn-3 position are both acylated, at about the same rate.
CAS REGISTRY NUMBER
COMMENTARY
9055-17-8
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
2-monooleoylglycerol + palmitoyl-CoA
2-oleoyl-3-palmitoylglycerol + CoA
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-
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?
acetyl-CoA + 2-oleoyl-(Z)-1-(octadec-9-enyl)glycerol
CoA + 2,3-dioleoyl-(Z)-1-(octadec-9-enyl)glycerol
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-
-
?
acetyl-CoA + 3-oleoyl-(Z)-1-(octadec-9-enyl)glycerol
CoA + 2,3-dioleoyl-(Z)-1-(octadec-9-enyl)glycerol
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-
-
?
acyl-CoA + 2-oleoylglycerol
CoA + 1-acyl-2-oleoylglycerol
deuterated substrate 2-oleoylglycerol-d5
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-
?
N-(7-nitro-2-1,3-benzoxadiazol-4-yl)amino-palmitoyl-CoA + 2-oleoylglycerol
CoA + N-(7-nitro-2-1,3-benzoxadiazol-4-yl)amino-palmitoyl-diacylglycerol
fluorescent-labeled substrate
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-
?
oleoyl-CoA + (Z)-1-(octadec-9-enyl)glycerol
CoA + 2-oleoyl-(Z)-1-(octadec-9-enyl)glycerol
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-
-
?
oleoyl-CoA + (Z)-1-(octadec-9-enyl)glycerol
CoA + 3-oleoyl-(Z)-1-(octadec-9-enyl)glycerol
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-
-
?
oleoyl-CoA + sn-2-monooleoylglycerol
CoA + sn-1,2(2,3)-dioleoylglycerol
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-
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-
?
palmitoyl-CoA + sn-2-monooleoylglycerol
CoA + 1(3)-palmitoyl-2-oleoylglycerol
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?
rac-1-linolenoylglycerol + oleoyl-CoA
1-linolenoyl-3-oleoylglycerol + CoA
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-
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?
rac-1-linoleoylglycerol + oleoyl-CoA
1-linoleoyl-3-oleoylglycerol + CoA
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-
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?
[N-[(7-nitro-2-1,3-benzoxadiazol-4-yl)-methyl]amino]palmitoyl-CoA + 2-oleoylglycerol
CoA + 1-[N-[(7-nitro-2-1,3-benzoxadiazol-4-yl)-methyl]amino]palmitoyl-2-oleoylglycerol
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-
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acyl-CoA + sn-2-monoacylglycerol
CoA + diacylglycerol
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representative enzyme of the neutral lipid pathway
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-
?
acyl-CoA + sn-2-monoacylglycerol
CoA + diacylglycerol
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the enzyme plays a major role in the absorption of dietary fat by catalyzing the resynthesis of triacylglycerol in enterocytes
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-
?
fatty acyl-CoA + sn-2-monoacylglycerol
CoA + 1,2-diacylglycerol
2-monoacylglycerol is preferred substrate
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?
additional information
?
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broad acyl-donor pattern with maximal activities for C10:0 to C16:0, the highest activity with C16:0. Preferential esterification for 2-monoacylglycerols as compared with the 1-isomers
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?
additional information
?
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the multifunctional enzyme plays an important role in lipid metabolism in human skin
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?
additional information
?
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isozyme DGAT1 also performs the reaction of the retinol O-fatty-acyltransferase, EC 2.3.1.76
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?
additional information
?
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the multifunctional O-acetyltransferase is catalyzing the reactions of the monoacylglycerol transferase, of the diacylglycerol transferase, EC 2.3.1.20, of the wax synthase, EC 2.3.1.75, and of the acyl-CoA:retinol acyltransferase, EC 2.3.1.76, overview
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-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
2-monooleoylglycerol + palmitoyl-CoA
2-oleoyl-3-palmitoylglycerol + CoA
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-
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?
additional information
?
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the multifunctional enzyme plays an important role in lipid metabolism in human skin
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-
?
acyl-CoA + sn-2-monoacylglycerol
CoA + diacylglycerol
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representative enzyme of the neutral lipid pathway
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-
?
acyl-CoA + sn-2-monoacylglycerol
CoA + diacylglycerol
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the enzyme plays a major role in the absorption of dietary fat by catalyzing the resynthesis of triacylglycerol in enterocytes
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-
?
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Mg2+
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(1r,4r)-4-([[(3,3,4,4,4-pentafluoro-2-methylbutan-2-yl)oxy]carbonyl]amino)cyclohexyl 5-[(4-chloro-2,6-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-1-carboxylate
compound shows strong selectivity for MGAT2 over DGAT1, DGAT2 and ACAT1
(1S)-4'-(2-cyclopropyl-3H-pyrrol-4-yl)-5'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-5-(4,4,4-trifluorobutoxy)-2,3-dihydro-1'H-spiro[indene-1,2'-pyridin]-6'(3'H)-one
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
(3R)-N-(2,4-difluorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
(6S)-4-(4-methylphenyl)-2-oxo-N-[4-(1H-tetrazol-5-yl)phenyl]-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-1,2,5,6-tetrahydropyridine-3-carboxamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
(6S)-4-(5-cyclopropyl-1,3-thiazol-2-yl)-6-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-3-(5-oxo-4,5-dihydro-1H-tetrazol-1-yl)-6-(trifluoromethyl)-5,6-dihydropyridin-2(1H)-one
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
(6S)-4-(5-cyclopropylthiophen-2-yl)-3-(2,5-dihydro-1H-tetrazol-5-yl)-6-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-5,6-dihydropyridin-2(1H)-one
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
(6S)-4-[4-(difluoromethyl)phenyl]-6-[2-fluoro-4-[(6,6,6-trifluorohexyl)oxy]phenyl]-N-(methanesulfonyl)-2-oxo-6-(trifluoromethyl)-1,2,5,6-tetrahydropyridine-3-carboxamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
1-(2,2,3,3,3-pentafluoropropyl)piperidin-4-yl 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxoimidazolidin-1-yl)-2,3-dihydro-1H-indole-1-carboxylate
ex hibits more than 100fold selectivity over human MGAT3, human DGAT1, and human DGAT2
1-([1,1'-biphenyl]-4-yl)-N-(2,4-difluorophenyl)-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-5-sulfonamide
ex hibits more than 100fold selectivity over human MGAT3, human DGAT1, and human DGAT2
1-[5-[(4-methoxyanilino)sulfanyl]-2-methylphenyl]-3-phenoxypropan-2-one
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
2-(4-chlorophenoxy)-N-[5-[(4-methoxyphenyl)sulfamoyl]-2-methylphenyl]acetamide
potent inhibitory activity toward human intestinal MGAT and recombinant human MGAT2, with selectivity over MGAT3. IC50 value in intestinal microsomes 0.000021 mM
2-(benzylsulfanyl)-6-[6-[4-(4-fluorophenyl)piperazin-1-yl]pyrimidin-4-yl]-3-phenyl-3,4,5,6,7,8-hexahydropyrido[4,3-d]pyrimidine
blocks MGAT2-mediated activity in vitro and in vivo
2-(cyclobutylsulfanyl)-3-phenyl-6-[([5-[4-(trifluoromethyl)phenoxy]pentyl]amino)acetyl]-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
2-(cyclobutylsulfanyl)-6-(3-[[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amino]propanoyl)-3-phenyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
2-(cyclobutylsulfanyl)-6-(3-[[(2,3-dihydro-1H-inden-2-yl)methyl]amino]propanoyl)-3-phenyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
2-[(1R)-1-(3,5-difluorophenyl)ethyl]-N-[3-(pyrrolidine-1-carbonyl)-1,2,4-oxadiazol-5-yl]-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
2-[2-(4-tert-butylphenyl)ethyl]-N-(4-fluorophenyl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
2-[2-(4-tert-butylphenyl)ethyl]-N-[4-(3-cyclopentylpropyl)-2-fluorophenyl]-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
2-[5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indol-1-yl]-N-(2,2,3,3,3-pentafluoropropyl)pyrimidine-5-carboxamide
ex hibits more than 100fold selectivity over human MGAT3, human DGAT1, and human DGAT2
3,3-dimethyl-2,5-dioxo-N-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
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3-(2,5-dihydro-1H-tetrazol-5-yl)-4-(5-ethylthiophen-2-yl)-6-[4-[(6,6,6-trifluorohexyl)oxy]-2-(trifluoromethyl)phenyl]pyridin-2(1H)-one
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
3-ethyl-2,5-dioxo-N-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
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3-ethyl-3-methyl-2,5-dioxo-N-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
3-ethyl-3-methyl-2,5-dioxo-N-[4-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
3-ethyl-N,3-dimethyl-2,5-dioxo-N-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
3-ethyl-N-(4-methoxyphenyl)-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
3-phenyl-2-[[(pyridin-3-yl)methyl]sulfanyl]-6-[5-(trifluoromethyl)-3a,4,5,6,7,7a-hexahydro-1H-benzimidazol-2-yl]-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-N-[4-(trifluoromethyl)phenyl]-2,3-dihydro-1H-indole-1-carboxamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
7-(4,6-di-tert-butylpyrimidin-2-yl)-3-[4-(trifluoromethoxy)phenyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
9-chloro-N-(2,4-difluorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
benzyl 2-[5-[(2,4-difluorophenyl)sulfamoyl]-7-(5-oxopyrazolidin-1-yl)-2,3-dihydro-1H-indol-1-yl]pyrimidine-5-carboxylate
ex hibits more than 100fold selectivity over human MGAT3, human DGAT1, and human DGAT2
ethyl 3-[4-([3-[2-(cyclohexylsulfanyl)-4-oxo-3-phenyl-3,5,7,8-tetrahydropyrido[4,3-d]pyrimidine-6(4H)-carbonyl]azetidin-1-yl]methyl)phenyl]propanoate
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
N-(2,4-dichlorophenyl)-2-[[(4-methoxyphenyl)methyl]amino]-4-oxo-3-phenyl-3,5,7,8-tetrahydropyrido[4,3-d]pyrimidine-6(4H)-carboxamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
N-(2,4-difluorophenyl)-3,3-diethyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
N-(2,4-difluorophenyl)-3,3-diethyl-N-methyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
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N-(2,4-difluorophenyl)-3,3-diethyl-N-methyl-2-oxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
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N-(2,4-difluorophenyl)-3,3-diethyl-N-methyl-5-oxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
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N-(2,4-difluorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
N-(2,4-difluorophenyl)-3-ethyl-N,3,4-trimethyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
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N-(2,4-difluorophenyl)-3-methyl-2,5-dioxo-3-propyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
N-(2,4-difluorophenyl)-7-(2-oxopyrrolidin-1-yl)-1-phenyl-2,3-dihydro-1H-indole-5-sulfonamide
ex hibits more than 100fold selectivity over human MGAT3, human DGAT1, and human DGAT2
N-(2-chlorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
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N-(3-chlorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
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N-(3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepin-7-yl)benzenesulfonamide
-
N-(4-chloro-2,6-difluorophenyl)-1-[5-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl]pyrimidin-2-yl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-5-sulfonamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
N-(4-chlorophenyl)-2,5-dioxo-1,2,4,5-tetrahydrospiro[1,4-benzodiazepine-3,1'-cyclobutane]-7-sulfonamide
-
N-(4-chlorophenyl)-2,5-dioxo-1,2,4,5-tetrahydrospiro[1,4-benzodiazepine-3,1'-cyclopentane]-7-sulfonamide
-
N-(4-chlorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
N-(4-chlorophenyl)-3-ethyl-N,1,3-trimethyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
N-(4-chlorophenyl)-N,3,3-trimethyl-5-oxo-2,3,4,5-tetrahydro-1,4-benzoxazepine-7-sulfonamide
-
N-(4-chlorophenyl)-N-methyl-2,5-dioxo-1,2,4,5-tetrahydrospiro[1,4-benzodiazepine-3,1'-cyclobutane]-7-carboxamide
-
N-benzyl-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
N-cyclohexyl-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
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N-[(1R)-1-(4-[[(2S)-2-(4-fluorophenyl)morpholin-4-yl]methyl]phenyl)ethyl]methanesulfonamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
N-[(1S)-1-[4-[(4-tert-butylpiperidin-1-yl)methyl]phenyl]-2,2,2-trifluoroethyl]methanesulfonamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
N-[(1S)-1-[4-[([[(3S)-2,3-dihydro[1,4]dioxino[2,3-b]pyridin-3-yl]methyl]amino)methyl]phenyl]2,2,2-trifluoroethyl]methanesulfonamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
N-[4-(difluoromethoxy)phenyl]-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
N-[5-[(2,4-difluorophenyl)sulfamoyl]-1-(2-phenylethyl)-2,3-dihydro-1H-indol-7-yl]acetamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
N-[[(6'S)-5-(2-hydroxypropan-2-yl)-2'-oxo-6'-[4-(4,4,4-trifluorobutoxy)phenyl]-6'-(trifluoromethyl)-1',2',5',6'-tetrahydro[2,4'-bipyridin]-3'-yl]methyl]-2-(methanesulfonyl)acetamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
XP620
-
selective isozyme DGAT1 inhibitor, inhibits the diacylglycerol acyltransferase and the retinol acyltransferase activities at the retinol recognition site
3-ethyl-3-methyl-2,5-dioxo-N-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
3-ethyl-3-methyl-2,5-dioxo-N-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
additional information
identification, development, and optimisation of a novel series of MGAT2 inhibitors, pIC50 values, overview
-
additional information
not inhibitory: acyl-CoA:diacylglycerol acyltransferase DGAT1 selective inhibitor XP-620
-
additional information
not inhibitory: acyl-CoA:diacylglycerol acyltransferase DGAT1 selective inhibitor XP-620
-
additional information
-
not inhibitory: acyl-CoA:diacylglycerol acyltransferase DGAT1 selective inhibitor XP-620
-
additional information
not inhibitory: acyl-CoA:diacylglycerol acyltransferase DGAT1 selective inhibitor XP-620, i.e (2R,3S,6R)-N-[2,6-di(propan-2-yl)phenyl]-3,6-dipentyl-3,6-dihydro-2H-thiopyran-2-carboxamide
-
additional information
not inhibitory: acyl-CoA:diacylglycerol acyltransferase DGAT1 selective inhibitor XP-620, i.e (2R,3S,6R)-N-[2,6-di(propan-2-yl)phenyl]-3,6-dipentyl-3,6-dihydro-2H-thiopyran-2-carboxamide
-
additional information
-
not inhibitory: acyl-CoA:diacylglycerol acyltransferase DGAT1 selective inhibitor XP-620, i.e (2R,3S,6R)-N-[2,6-di(propan-2-yl)phenyl]-3,6-dipentyl-3,6-dihydro-2H-thiopyran-2-carboxamide
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
additional information
additional information
-
inhibition kinetics depend highly on retinol concentration, overview, recombinant enzyme
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0000081
(1r,4r)-4-([[(3,3,4,4,4-pentafluoro-2-methylbutan-2-yl)oxy]carbonyl]amino)cyclohexyl 5-[(4-chloro-2,6-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-1-carboxylate
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000001
(1S)-4'-(2-cyclopropyl-3H-pyrrol-4-yl)-5'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-5-(4,4,4-trifluorobutoxy)-2,3-dihydro-1'H-spiro[indene-1,2'-pyridin]-6'(3'H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000063
(3R)-N-(2,4-difluorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000007
(6S)-4-(4-methylphenyl)-2-oxo-N-[4-(1H-tetrazol-5-yl)phenyl]-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-1,2,5,6-tetrahydropyridine-3-carboxamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000002
(6S)-4-(5-cyclopropyl-1,3-thiazol-2-yl)-6-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-3-(5-oxo-4,5-dihydro-1H-tetrazol-1-yl)-6-(trifluoromethyl)-5,6-dihydropyridin-2(1H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000002
(6S)-4-(5-cyclopropylthiophen-2-yl)-3-(2,5-dihydro-1H-tetrazol-5-yl)-6-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-5,6-dihydropyridin-2(1H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000001
(6S)-4-[4-(difluoromethyl)phenyl]-6-[2-fluoro-4-[(6,6,6-trifluorohexyl)oxy]phenyl]-N-(methanesulfonyl)-2-oxo-6-(trifluoromethyl)-1,2,5,6-tetrahydropyridine-3-carboxamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000067
1-(2,2,3,3,3-pentafluoropropyl)piperidin-4-yl 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxoimidazolidin-1-yl)-2,3-dihydro-1H-indole-1-carboxylate
Homo sapiens
pH 7.4, 23°C
0.0000014
1-([1,1'-biphenyl]-4-yl)-N-(2,4-difluorophenyl)-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-5-sulfonamide
Homo sapiens
pH 7.4, 23°C
0.00013
1-[5-[(4-methoxyanilino)sulfanyl]-2-methylphenyl]-3-phenoxypropan-2-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000083
2-(4-chlorophenoxy)-N-[5-[(4-methoxyphenyl)sulfamoyl]-2-methylphenyl]acetamide
Homo sapiens
pH 7.5, 23°C
0.000075
2-(benzylsulfanyl)-6-[6-[4-(4-fluorophenyl)piperazin-1-yl]pyrimidin-4-yl]-3-phenyl-3,4,5,6,7,8-hexahydropyrido[4,3-d]pyrimidine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00000064
2-(cyclobutylsulfanyl)-3-phenyl-6-[([5-[4-(trifluoromethyl)phenoxy]pentyl]amino)acetyl]-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000011
2-(cyclobutylsulfanyl)-6-(3-[[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amino]propanoyl)-3-phenyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00000038
2-(cyclobutylsulfanyl)-6-(3-[[(2,3-dihydro-1H-inden-2-yl)methyl]amino]propanoyl)-3-phenyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000016
2-[(1R)-1-(3,5-difluorophenyl)ethyl]-N-[3-(pyrrolidine-1-carbonyl)-1,2,4-oxadiazol-5-yl]-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.001522
2-[2-(4-tert-butylphenyl)ethyl]-N-(4-fluorophenyl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000028
2-[2-(4-tert-butylphenyl)ethyl]-N-[4-(3-cyclopentylpropyl)-2-fluorophenyl]-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000051
2-[5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indol-1-yl]-N-(2,2,3,3,3-pentafluoropropyl)pyrimidine-5-carboxamide
Homo sapiens
pH 7.4, 23°C
0.0000003
3-(2,5-dihydro-1H-tetrazol-5-yl)-4-(5-ethylthiophen-2-yl)-6-[4-[(6,6,6-trifluorohexyl)oxy]-2-(trifluoromethyl)phenyl]pyridin-2(1H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000398
3-ethyl-3-methyl-2,5-dioxo-N-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000056
3-phenyl-2-[[(pyridin-3-yl)methyl]sulfanyl]-6-[5-(trifluoromethyl)-3a,4,5,6,7,7a-hexahydro-1H-benzimidazol-2-yl]-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000034
5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-N-[4-(trifluoromethyl)phenyl]-2,3-dihydro-1H-indole-1-carboxamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000019
7-(4,6-di-tert-butylpyrimidin-2-yl)-3-[4-(trifluoromethoxy)phenyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000009
9-chloro-N-(2,4-difluorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000034
benzyl 2-[5-[(2,4-difluorophenyl)sulfamoyl]-7-(5-oxopyrazolidin-1-yl)-2,3-dihydro-1H-indol-1-yl]pyrimidine-5-carboxylate
Homo sapiens
pH 7.4, 23°C
0.000004
ethyl 3-[4-([3-[2-(cyclohexylsulfanyl)-4-oxo-3-phenyl-3,5,7,8-tetrahydropyrido[4,3-d]pyrimidine-6(4H)-carbonyl]azetidin-1-yl]methyl)phenyl]propanoate
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000032
N-(2,4-difluorophenyl)-7-(2-oxopyrrolidin-1-yl)-1-phenyl-2,3-dihydro-1H-indole-5-sulfonamide
Homo sapiens
pH 7.4, 23°C
0.0000078
N-(4-chloro-2,6-difluorophenyl)-1-[5-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl]pyrimidin-2-yl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-5-sulfonamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000274
N-[(1R)-1-(4-[[(2S)-2-(4-fluorophenyl)morpholin-4-yl]methyl]phenyl)ethyl]methanesulfonamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000058
N-[(1S)-1-[4-[(4-tert-butylpiperidin-1-yl)methyl]phenyl]-2,2,2-trifluoroethyl]methanesulfonamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000038
N-[(1S)-1-[4-[([[(3S)-2,3-dihydro[1,4]dioxino[2,3-b]pyridin-3-yl]methyl]amino)methyl]phenyl]2,2,2-trifluoroethyl]methanesulfonamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000001
N-[5-[(2,4-difluorophenyl)sulfamoyl]-1-(2-phenylethyl)-2,3-dihydro-1H-indol-7-yl]acetamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00000073
N-[[(6'S)-5-(2-hydroxypropan-2-yl)-2'-oxo-6'-[4-(4,4,4-trifluorobutoxy)phenyl]-6'-(trifluoromethyl)-1',2',5',6'-tetrahydro[2,4'-bipyridin]-3'-yl]methyl]-2-(methanesulfonyl)acetamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.4
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
expression of MOGAT2 does not correlate with enzymatic activity
expression of MOGAT2 does not correlate with enzymatic activity
expression of MOGAT3 is correlated with enzymatic activity
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
integral membrane protein, the C-terminus is exposed to the cytosol, while the N-terminus is partially buried in the ER membrane. Domains that are important for catalysis face the cytosol. Both transmembrane domains of MGAT2 are important for its ER localization, and MGAT2 is present in mitochondrial-associated membranes
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
evolution
three subtypes of monoacylglycerol O-acyltransferase, MGAT, enzymes, MGAT1, MGAT2, and MGAT3: in a phylogenetic tree with inferred evolutionary relationships, MGAT3 shares higher sequence homology with the diacylglycerol O-acyltransferase 2 enzyme than with MGAT1 or MGAT2, phylogenetic analysis
malfunction
the enzyme is involved in hepatic steatosis, characterized by an increase in intrahepatic triacylglycerol, is an important marker of metabolic dysfunction and is associated closely with insulin resistance and dyslipidemia. Inhibition of MGAT1 ameliorates hepatic steatosis in human liver Hep-G2 cell line, inhibition of MGAT1 by siRNA treatment efficiently ameliorates the lipid accumulation
metabolism
the enzyme is involved in triglyceride synthesis by catalyzing the formation of diacylglycerol from monoacylglycerol and fatty acyl CoAs
physiological function
monoacylglycerol O-acyltransferase 1 is regulated by peroxisome proliferator-activated receptor gamma in human hepatocytes and increases lipid accumulation
evolution
the enzyme belongs to the evolutionarily conserved acyltransferase gene family. All DGAT2 family members, including monoacylglycerol acyltransferases (MGAT)1-3 and wax synthases 1 and 2, contain a highly conserved four amino acid sequence - histidine-proline-histidine-glycine
malfunction
knockout of MOGAT3 attenuates MGAT activity in a liver-derived cell line
metabolism
the enzyme interacts with the acyl CoA:1,2-diacylglycerol acyltransferase (DGAT)-2, an endoplasmic reticulum integral membrane protein that catalyzes triacylglycerol synthesis using diacylglycerol and fatty acyl CoA as substrates. Deletion mutagenesis shows that the interaction with MGAT2 is dependent on the two transmembrane domains of DGAT2. The interaction of the enzyme and DGAT2 serves to channel lipid substrates efficiently for triacylglycerol biosynthesis
physiological function
physiological function
acyl CoA:monoacylglycerol acyltransferase (MGAT) catalyzes the resynthesis of triacylglycerol, a crucial step in the absorption of dietary fat. MGAT2 in the intestine plays an indispensable role in enhancing metabolic efficiency, in other tissues it may contribute to the regulation of energy metabolism
physiological function
in the intestine, the majority of diacylglycerol is produced by the MGAT pathway via monoacylglycerol acyltransferase-2, MGAT2, which catalyzes the synthesis of diacylglycerol in an acyl CoA-dependent manner using 2-monoacylglycerol as an acyl acceptor. Co-expression of acyl CoA:1,2-diacylglycerol acyltransferase, DGAT2, and monoacylglycerol acyltransferase MGAT2 stimulates triacylglycerol storage
physiological function
the enzyme is involved in diabetes, obesity and other diseases which together constitute the metabolic syndrome
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). MOGT1_HUMAN
335
1
38812
Swiss-Prot
Secretory Pathway (Reliability: 3)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
160000
the enzyme exists as both a homodimer and homotetramer, cross-linking
80000
the enzyme exists as both a homodimer and homotetramer, cross-linking
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
C334A
located at the extreme C-terminus, about 200% of wild-type activity
additional information
additional information
mice lacking the gene Mogat2 , which codes for an MGAT highly expressed in the small intestine, are resistant to obesity and other metabolic disorders induced by high-fat feeding. The Mogat2-deficient mice absorb normal amounts of dietary fat but exhibit a reduced rate of fat absorption, increased energy expenditure, decreased respiratory exchange ratio, and impaired metabolic efficiency. Recombinant expression of the human gene MOGAT2, encoding the enzyme, in the intestine increases intestinal MGAT activity, restores fat absorption rate, partially corrects energy expenditure, and promotes weight gain upon high-fat feeding. The changes in respiratory exchange ratio are not reverted, and the recoveries in metabolic efficiency and weight gain are incomplete
additional information
-
mice lacking the gene Mogat2 , which codes for an MGAT highly expressed in the small intestine, are resistant to obesity and other metabolic disorders induced by high-fat feeding. The Mogat2-deficient mice absorb normal amounts of dietary fat but exhibit a reduced rate of fat absorption, increased energy expenditure, decreased respiratory exchange ratio, and impaired metabolic efficiency. Recombinant expression of the human gene MOGAT2, encoding the enzyme, in the intestine increases intestinal MGAT activity, restores fat absorption rate, partially corrects energy expenditure, and promotes weight gain upon high-fat feeding. The changes in respiratory exchange ratio are not reverted, and the recoveries in metabolic efficiency and weight gain are incomplete
additional information
a mutant lacking all five cysteine residues is devoid of monoacylglycerol acyltransferase activity
additional information
-
a mutant lacking all five cysteine residues is devoid of monoacylglycerol acyltransferase activity
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
MGAT1 gene expression analysis by real-time PCR, the MGAT1 promoter is highly regulated by PPARgamma, phylogenetic analysis
chromosomal location, expression of the FLAG-tagged enzyme in Spodoptera frugiperda Sf9 cells and in COS-7 cells
-
gene MOGAT, co-expression of enzyme MGAT2 and acyl CoA:1,2-diacylglycerol acyltransferase, DGAT2, in HEK-293T and in COS-7 cells and co-localization in the endoplasmic reticulum and on lipid droplets
gene MOGAT, expression analysis, recombinant expression in enzyme-deficient mice
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
expression of MGAT1 is robustly induced during adipocyte differentiation and its expression is suppressed in metabolically abnormal obese human subjects
isozyme MGAT1 is highly induced up to 10fold by peroxisome proliferator-activated receptor gamma, PPARgamma, overexpression in human primary hepatocytes
marked weight loss following gastric bypass surgery is associated with a significant reduction in MOGAT2 and MOGAT3 expression
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
medicine
expression of MGAT1 is robustly induced during adipocyte differentiation and its expression is suppressed in metabolically abnormal obese human subjects
analysis
drug development
[acyl CoA]monoacylglycerol acyltransferase 2 (MGAT2) is of interest as a target for therapeutic treatment of diabetes, obesity and other diseases which together constitute the metabolic syndrome
pharmacology
[acyl CoA]monoacylglycerol acyltransferase 2 (MGAT2) is of interest as a target for therapeutic treatment of diabetes, obesity and other diseases which together constitute the metabolic syndrome
analysis
development of a MGAT enzymatic assay of human intestinal microsomes using a high-throughput mass spectrometry-based detection system
analysis
development of LC/ESI/MS/MS-based fat absorption assay using 1-oleoyl-glycerol-d5 and U13C-triglyceride to assess the ability of MGAT2 inhibitors to inhibit fat absorption in CD1 mice by a meal tolerance test
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Loirdighi, N.; Menard, D.; Delvin, E.; Levy, E.
Ontogeny and location of HMG-CoA reductase, ACAT, and MGAT in human small intestine
Am. J. Physiol.
273
G62-G67
1997
Homo sapiens
Bierbach, H.
Triacylglycerol biosynthesis in human small intestinal mucosa. Acyl-CoA: monoglyceride acyltransferase
Digestion
28
138-147
1983
Homo sapiens
Yen, C.L.; Farese, R.V., Jr.
MGAT2, a monoacylglycerol acyltransferase expressed in the small intestine
J. Biol. Chem.
5
1-24
2003
Homo sapiens, Mus musculus
-
Lockwood, J.F.; Cao, J.; Burn, P.; Shi, Y.
Human intestinal monoacylglycerol acyltransferase: differential features in tissue expression and activity
Am. J. Physiol.
285
E927-937
2003
Homo sapiens (Q3SYC2), Homo sapiens
Cheng, D.; Nelson, T.C.; Chen, J.; Walker, S.G.; Wardwell-Swanson, J.; Meegalla, R.; Taub, R.; Billheimer, J.T.; Ramaker, M.; Feder, J.N.
Identification of acyl coenzyme A:monoacylglycerol acyltransferase 3, an intestinal specific enzyme implicated in dietary fat absorption
J. Biol. Chem.
278
13611-13614
2003
Homo sapiens (Q86VF5), Homo sapiens
Yen, C.L.; Brown Iv, C.H.; Monetti, M.; Farese, R.V., Jr.
A human skin multifunctional O-acyltransferase that catalyzes the synthesis of acylglycerols, waxes, and retinyl esters
J. Lipid Res.
46
2388-2397
2005
Homo sapiens
Orland, M.D.; Anwar, K.; Cromley, D.; Chu, C.; Chen, L.; Billheimer, J.T.; Hussain, M.M.; Cheng, D.
Acyl coenzyme A dependent retinol esterification by acyl coenzyme A:diacylglycerol acyltransferase 1
Biochim. Biophys. Acta
1737
76-82
2005
Homo sapiens
Hall, A.M.; Kou, K.; Chen, Z.; Pietka, T.A.; Kumar, M.; Korenblat, K.M.; Lee, K.; Ahn, K.; Fabbrini, E.; Klein, S.; Goodwin, B.; Finck, B.N.
Evidence for regulated monoacylglycerol acyltransferase expression and activity in human liver
J. Lipid Res.
53
990-999
2012
Homo sapiens (Q3SYC2), Homo sapiens (Q86VF5), Homo sapiens (Q96PD6), Homo sapiens
Yu, J.H.; Lee, Y.J.; Kim, H.J.; Choi, H.; Choi, Y.; Seok, J.W.; Kim, J.W.
Monoacylglycerol O-acyltransferase 1 is regulated by peroxisome proliferator-activated receptor gamma in human hepatocytes and increases lipid accumulation
Biochem. Biophys. Res. Commun.
460
715-720
2015
Homo sapiens (Q96PD6), Homo sapiens
Barlind, J.G.; Buckett, L.K.; Crosby, S.G.; Davidsson, O.e.; Emtenaes, H.; Ertan, A.; Jurva, U.; Lemurell, M.; Gutierrez, P.M.; Nilsson, K.; OMahony, G.; Petersson, A.U.; Redzic, A.; Wagberg, F.; Yuan, Z.Q.
Identification and design of a novel series of MGAT2 inhibitors
Bioorg. Med. Chem. Lett.
23
2721-2726
2013
Homo sapiens (Q3SYC2)
Jin, Y.; McFie, P.J.; Banman, S.L.; Brandt, C.; Stone, S.J.
Diacylglycerol acyltransferase-2 (DGAT2) and monoacylglycerol acyltransferase-2 (MGAT2) interact to promote triacylglycerol synthesis
J. Biol. Chem.
289
28237-28248
2014
Homo sapiens (Q3SYC2)
Gao, Y.; Nelson, D.W.; Banh, T.; Yen, M.I.; Yen, C.L.
Intestine-specific expression of MOGAT2 partially restores metabolic efficiency in Mogat2-deficient mice
J. Lipid Res.
54
1644-1652
2013
Homo sapiens (Q3SYC2), Homo sapiens, Mus musculus (Q80W94), Mus musculus C57/BL6J (Q80W94)
Qi, J.; Lang, W.; Connelly, M.A.; Du, F.; Liang, Y.; Caldwell, G.W.; Martin, T.; Hansen, M.K.; Kuo, G.H.; Gaul, M.D.; Pocai, A.; Lee, S.
Metabolic tracing of monoacylglycerol acyltransferase-2 activity in vitro and in vivo
Anal. Biochem.
524
68-75
2017
Homo sapiens (Q3SYC2), Homo sapiens
McFie, P.J.; Izzard, S.; Vu, H.; Jin, Y.; Beauchamp, E.; Berthiaume, L.G.; Stone, S.J.
Membrane topology of human monoacylglycerol acyltransferase-2 and identification of regions important for its localization to the endoplasmic reticulum
Biochim. Biophys. Acta
1861
1192-1204
2016
Homo sapiens (Q3SYC2), Homo sapiens
Adachi, R.; Ishii, T.; Ogawa, K.; Matsumoto, S.; Satou, T.; Sakamoto, J.; Sato, K.; Kawamoto, T.
Pharmacological characterization of a series of aryl-sulfonamide derivatives that potently and selectively inhibit monoacylglycerol acyltransferase 2
Eur. J. Pharmacol.
791
569-577
2016
Homo sapiens (Q3SYC2), Homo sapiens, Mus musculus (Q80W94), Mus musculus
Mochida, T.; Take, K.; Maki, T.; Nakakariya, M.; Adachi, R.; Sato, K.; Kitazaki, T.; Takekawa, S.
Inhibition of MGAT2 modulates fat-induced gut peptide release and fat intake in normal mice and ameliorates obesity and diabetes in ob/ob mice fed on a high-fat diet
FEBS Open Bio
10
316-326
2020
Homo sapiens (Q3SYC2), Mus musculus (Q80W94)
Ma, Z.; Onorato, J.M.; Chen, L.; Nelson, D.W.; Yen, C.E.; Cheng, D.
Synthesis of neutral ether lipid monoalkyl-diacylglycerol by lipid acyltransferases
J. Lipid Res.
58
1091-1099
2017
Homo sapiens (Q3SYC2), Homo sapiens (Q86VF5), Homo sapiens
Liss, K.H.H.; Lutkewitte, A.J.; Pietka, T.; Finck, B.N.; Franczyk, M.; Yoshino, J.; Klein, S.; Hall, A.M.
Metabolic importance of adipose tissue monoacylglycerol acyltransferase 1 in mice and humans
J. Lipid Res.
59
1630-1639
2018
Homo sapiens (Q96PD6), Homo sapiens, Mus musculus (Q91ZV4)
Devasthale, P.; Cheng, D.
Monoacylglycerol acyltransferase 2 (MGAT2) inhibitors for the treatment of metabolic diseases and nonalcoholic steatohepatitis (NASH)
J. Med. Chem.
61
9879-9888
2018
Homo sapiens (Q3SYC2), Mus musculus (Q80W94)
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