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2.3.1.22: 2-acylglycerol O-acyltransferase

This is an abbreviated version!
For detailed information about 2-acylglycerol O-acyltransferase, go to the full flat file.

Word Map on EC 2.3.1.22

Reaction

acyl-CoA
+
2-acylglycerol
=
CoA
 +
diacylglycerol

Synonyms

acyl CoA:monoacylglycerol acyltransferase, acyl CoA:monoacylglycerol acyltransferase-2, acyl coenzyme A-monoglyceride acyltransferase, acyl coenzyme A:diacylglycerol acyltransferase, acyl-CoA:monoacylglycerol acyltransferase, acyl-CoA:monoacylglycerol transferase, acyl-coenzyme A:monoacylglycerol acyltransferase, acylglycerol palmitoyltransferase, DGAT, DGAT1/ARAT, diacylglycerol acyltransferase, GPAT4, LPGAT1, lysophosphatidylglycerol acyltransferase 1, MFAT, MGAT, MGAT1, Mgat2, MGAT3, MGOT1, MGOT2, MGOT3, MOGAT1, MOGAT2, MOGAT3, monoacylglycerol acyltransferase, monoacylglycerol acyltransferase-2, monoacylglycerol O-acyltransferase, monoacylglycerol O-acyltransferase 1, monoglyceride acyltransferase, More, multifunctional O-acyltransferase, OLE3, oleosin 3, palmitoyltransferase, acylglycerol, wax ester synthase/acyl coenzyme A:diacylglycerol acyltransferase, WS/DGAT, [acyl CoA]monoacylglycerol acyltransferase 2

ECTree

     2 Transferases
         2.3 Acyltransferases
             2.3.1 Transferring groups other than aminoacyl groups
                2.3.1.22 2-acylglycerol O-acyltransferase

Inhibitors

Inhibitors on EC 2.3.1.22 - 2-acylglycerol O-acyltransferase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
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
(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
(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
1-([1,1'-biphenyl]-4-yl)-N-(2,4-difluorophenyl)-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-5-sulfonamide
1-[5-[(4-methoxyanilino)sulfanyl]-2-methylphenyl]-3-phenoxypropan-2-one
MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis
2,4,6-Trinitrobenzene sulfonic acid
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-monooleoylglycerol
-
high concentration
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
2-[2-(4-tert-butylphenyl)ethyl]-N-[4-(3-cyclopentylpropyl)-2-fluorophenyl]-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide
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
3,3-dimethyl-2,5-dioxo-N-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
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
-
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
5,5'-dithiobis-(2-nitrobenzoic acid)
-
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
acetone
-
10%, liver
benzyl 2-[5-[(2,4-difluorophenyl)sulfamoyl]-7-(5-oxopyrazolidin-1-yl)-2,3-dihydro-1H-indol-1-yl]pyrimidine-5-carboxylate
beta-octylglucoside
bovine serum albumin
-
Ca2+
-
14% inhibition at 2.5 mM
CaCl2
-
12.5 mM, 20-30% inhibition
CHAPS
deoxycholate
-
inhibition of liver enzyme
diethyldicarbonate
-
0.04 mM, 50% inhibition, 0.05 mM palmitate partly protects, completely reversible by 50 mM hydroxylamine, enzyme from intestine is less sensitive than enzyme from liver
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
HgCl2
KI
-
300 mM, 30% inhibition
Mg2+
-
66% inhibition at 8 mM
Mn2+
-
85.5% inhibition at 2.5 mM, inhibition of Mg2+ and bovine serum albumin is antagonistic
MnCl2
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
-
N-(2,4-difluorophenyl)-3,3-diethyl-N-methyl-2-oxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
N-(2,4-difluorophenyl)-3,3-diethyl-N-methyl-5-oxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
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
-
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
N-(2-chlorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
N-(3-chlorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide
-
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
-
N-ethylmaleimide
-
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
NEM
-
2 mM, 12% inhibition
oleic acid
-
-
palmitoyl-CoA
phytosphingosine
-
-
shRNA-adenovirus
-
short hairpin RNA adenovirus construct to knockdown mouse lysophosphatidylglycerol acyltransferase 1, injected via tail vein
-
sphinganine
-
-
sphingosine
-
IC50 is 9 mol%, inhibits activity in Triton X-100 mixed micelles and isolated hepatocytes
Stearylamine
-
-
taurocholate
Triton X-100
XP620
-
selective isozyme DGAT1 inhibitor, inhibits the diacylglycerol acyltransferase and the retinol acyltransferase activities at the retinol recognition site
additional information
-