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Information on EC 2.3.1.20 - diacylglycerol O-acyltransferase and Organism(s) Homo sapiens and UniProt Accession O75907

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EC Tree
IUBMB Comments
Palmitoyl-CoA and other long-chain acyl-CoAs can act as donors.
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Select one or more organisms in this record: ?
This record set is specific for:
Homo sapiens
UNIPROT: O75907
Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea
Synonyms
1,2-diacylglycerol acyltransferase, 2 diacylglycerol acyltransferase, ACY99349, acyl CoA:1,2-diacylglycerol acyltransferase, acyl CoA:diacylglycerol acyltransferase, acyl CoA:diacylglycerol acyltransferase 1, acyl CoA:diacylglycerol acyltransferase-2, acyl coenzyme A:diacylglycerol acyltransferase, acyl coenzyme A:diacylglycerol acyltransferase 1, acyl coenzyme A:diacylglycerol acyltransferase 2, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
1,2-diacylglycerol acyltransferase
-
-
-
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acyl CoA:1,2-diacylglycerol acyltransferase
247
-
acyl CoA:diacylglycerol acyltransferase
247
-
acyl coenzyme A:diacylglycerol acyltransferase 1
247
-
acyl coenzyme A:diacylglycerol acyltransferase 2
247
-
acyl-CoA:1,2-dioleoyl-sn-glycerol acyltransferase
-
-
-
-
acyl-CoA:diacylglycerol acyltransferase
280819, 280820
-
acyl-CoA:diacylglycerol acyltransferase 1
290195
-
acyl-CoA:diacylglycerol acyltransferase 2
acyltransferase, diacylglycerol
-
-
-
-
DC3
280820
-
DGAT-1
DGAT1
DGAT1A
-
-
-
-
DGAT2
DGAT2A
-
-
-
-
diacylglycerol acyltransferase
diacylglycerol acyltransferase 1
diacylglycerol acyltransferase 2
247
-
diacylglycerol acyltransferase type 1
247
-
diacylglycerol acyltransferase-2
247
-
diglyceride acyltransferase
-
-
-
-
diglyceride O-acyltransferase
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-
-
-
MFAT
247
-
MGAT
247
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multifunctional O-acyltransferase
247
-
palmitoyl-CoA-sn-1,2-diacylglycerol acyltransferase
-
-
-
-
additional information
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Acyl group transfer
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-
-
-
SYSTEMATIC NAME
IUBMB Comments
acyl-CoA:1,2-diacyl-sn-glycerol O-acyltransferase
Palmitoyl-CoA and other long-chain acyl-CoAs can act as donors.
CAS REGISTRY NUMBER
COMMENTARY hide
9029-98-5
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
acyl-CoA + 1,2-diacyl-sn-glycerol
CoA + 1,2,3-triacylglycerol
show the reaction diagram
-
-
-
?
palmitoyl-CoA + 1,2-dioleoyl-sn-glycerol
CoA + 1,2-dioleoyl-3-palmitoyl-sn-glycerol
show the reaction diagram
-
-
-
?
1,2-dioleoylglycerol + arachidonoyl-CoA
1,2-dioleoyl-3-arachidonoylglycerol + CoA
show the reaction diagram
-
about 8% of the activity with palmitoyl-CoA
-
-
?
1,2-dioleoylglycerol + linoleoyl-CoA
1,2-dioleoyl-3-linoleoylglycerol + CoA
show the reaction diagram
-
about 12% of the activity with palmitoyl-CoA
-
-
?
1,2-dioleoylglycerol + oleoyl-CoA
triolein + CoA
show the reaction diagram
1,2-dioleoylglycerol + palmitoyl-CoA
1,2-dioleoyl-3-palmitoylglycerol + CoA
show the reaction diagram
-
-
-
-
?
1,2-dioleoylglycerol + stearoyl-CoA
1,2-dioleoyl-3-stearoylglycerol + CoA
show the reaction diagram
-
about 10% of the activity with palmitoyl-CoA
-
-
?
acyl-CoA + 1,2-diacyl-sn-glycerol
CoA + 1,2,3-triacylglycerol
show the reaction diagram
-
-
-
-
?
acyl-CoA + 1,2-diacyl-sn-glycerol
CoA + triacylglycerol
show the reaction diagram
-
-
-
-
?
acyl-CoA + 1,2-diacylglycerol
CoA + triacylglycerol
show the reaction diagram
acyl-CoA + 2-monoacylglycerol
CoA + diacylglycerol
show the reaction diagram
-
-
-
-
?
acyl-CoA + hexadecanol
CoA + ?
show the reaction diagram
-
-
-
-
?
linoleoyl-CoA + 1,2-diacylglycerol
CoA + 1,2-diacyl-3-linoleoylglycerol
show the reaction diagram
myristoyl-CoA + 1,2-diacylglycerol
CoA + 1,2-diacyl-3-myristoylglycerol
show the reaction diagram
-
-
-
-
?
octanoyl-CoA + 1,2-di-(cis-9-octadecenoyl)-sn-glycerol
CoA + 1,2-di-(cis-9-octadecenoyl)-3-octanoyl-sn-glycerol
show the reaction diagram
-
-
-
-
?
oleoyl-CoA + 1,2-dioleoyl-sn-glycerol
CoA + triolein
show the reaction diagram
-
-
-
-
?
oleoyl-CoA + 1,2-dioleoyl-sn-glycerol
CoA + trioleoylglycerol
show the reaction diagram
-
-
-
-
?
oleoyl-CoA + sn-1,2-dioleoylglycerol
triolein + CoA
show the reaction diagram
-
-
-
-
?
oleoyl-CoA + sn-2-monooleoylglycerol
CoA + 1,2-dioleoyl-sn-glycerol
show the reaction diagram
-
-
-
-
?
palmitoyl-CoA + 1,2-dioleoyl-sn-glycerol
CoA + 1,2-dioleoyl-3-palmitoyl-sn-glycerol
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
acyl-CoA + 1,2-diacyl-sn-glycerol
CoA + 1,2,3-triacylglycerol
show the reaction diagram
-
-
-
?
1,2-dioleoylglycerol + palmitoyl-CoA
1,2-dioleoyl-3-palmitoylglycerol + CoA
show the reaction diagram
-
-
-
-
?
acyl-CoA + 1,2-diacyl-sn-glycerol
CoA + 1,2,3-triacylglycerol
show the reaction diagram
-
-
-
-
?
acyl-CoA + 1,2-diacyl-sn-glycerol
CoA + triacylglycerol
show the reaction diagram
-
-
-
-
?
acyl-CoA + 1,2-diacylglycerol
CoA + triacylglycerol
show the reaction diagram
-
last step of triacylglycerol synthesis
-
-
?
acyl-CoA + 2-monoacylglycerol
CoA + diacylglycerol
show the reaction diagram
-
-
-
-
?
octanoyl-CoA + 1,2-di-(cis-9-octadecenoyl)-sn-glycerol
CoA + 1,2-di-(cis-9-octadecenoyl)-3-octanoyl-sn-glycerol
show the reaction diagram
-
-
-
-
?
additional information
?
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the multifunctional enzyme plays an important role in lipid metabolism in human skin
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-
?
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mg2+
required
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1R,2R)-2-[4'-[(phenylcarbamoyl)amino][1,1'-biphenyl]-4-carbonyl]cyclopentane-1-carboxylic acid
-
(4-[4-[4-(2-amino-5-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
(4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
(4-[4-[4-(5-chloro-2-nitrobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
(4-[4-[4-([[2-fluoro-5-(trifluoromethyl)phenyl]carbamoyl]amino)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
(4S,7R)-4-(5,5-dimethyl-4-oxo-4,5-dihydrofuran-2-yl)-2,2-dimethyl-4,7-bis[(4E)-4-methyl-5-[(2R)-4-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl]pent-4-en-1-yl]-4,5,6,7-tetrahydro-1-benzofuran-3(2H)-one
89.23% inhibition
3,5-dimethyl-6-([(6E)-6-methyl-7-[(2S)-4-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl]hept-6-en-1-yl]oxy)pyrazine-2-carboxamide
-
3-(4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)propanoic acid
-
4-amino-6-[(4E)-4-methyl-5-[(2R)-4-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl]pent-4-en-2-yn-1-yl]-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5(6H)-one
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4-amino-6-[(4E)-4-methyl-5-[(2S)-4-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl]pent-4-en-2-yn-1-yl]-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5(6H)-one
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4-[4-(4-[[2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carbonyl]amino]phenyl)piperidine-1-carbonyl]cyclohexane-1-carboxylic acid
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4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexane-1-carboxylic acid
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amidepsine A
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amidepsine B
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amidepsine C
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amidepsine D
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cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
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cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetic acid
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methyl 2-(4-(4-(4-((tert-butoxycarbonyl)amino)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohex-3-en-1-yl)acetate
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methyl 2-(4-(4-(4-((tert-butoxycarbonyl)amino)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl) acetate
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methyl 2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
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methyl 2-(4-(4-(4-aminophenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
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methyl cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
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methyl trans-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
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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
roselipin 1a
-
roselipin 1B
-
roselipin 2A
-
roselipin 2B
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tert-butyl (4-(7-bromothieno[3,2-d]pyrimidin-4-yl)phenyl)carbamate
-
trans-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
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trans-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetic acid
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[(1r,4r)-4-(4-[[5-(3,4-difluoroanilino)-1,3,4-oxadiazole-2-carbonyl]amino]phenyl)cyclohexyl]acetic acid
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[(1r,4r)-4-[4-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]cyclohexyl]acetic acid
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[(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
-
[(1r,4r)-4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl]acetic acid
89.32% inhibition
[4-(4-[4-[(naphthalene-2-carbonyl)amino]phenyl]thieno[3,2-d]pyrimidin-7-yl)cyclohexyl]acetic acid
-
[4-[4-(4-[[(3-chlorophenyl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
[4-[4-(4-[[(4-chloropyridin-2-yl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
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[4-[4-(4-[[(5-bromopyridin-3-yl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
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[4-[4-(4-[[2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carbonyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
[4-[4-(4-[[6-(trifluoromethyl)pyridine-3-carbonyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
(2S)-1-(3-[[(2S)-1-ethoxy-4-phenylbutan-2-yl]sulfamoyl]anilino)-4-methyl-1-oxopentan-2-yl 2,2-dimethylpropanoate
-
-
(2S)-1-[(1-[[(1S)-1-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-3-phenylpropyl]carbamoyl]cyclopentyl)amino]-4-methyl-1-oxopentan-2-yl 2,2-dimethylpropanoate
-
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(trans-4-(4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
-
inhibitor displays good metabolic stability and high intestinal permeability values
(trans-4-(4-[(5-cyclopentylethyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
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(trans-4-(4-[(5-cyclopentylmethyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
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(trans-4-(4-[(5-[1-fluorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
-
inhibitor displays good metabolic stability and high intestinal permeability values
(trans-4-(4-[(5-[2-chlorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
-
inhibitor displays good metabolic stability and high intestinal permeability values
(trans-4-(4-[(5-[2-fluorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
-
inhibitor displays good metabolic stability and high intestinal permeability values
(trans-4-[4-[(3-benzyl-1,2,4-oxadiazol-5-yl)carbamoyl]phenyl]cyclohexyl)acetic acid
-
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(trans-4-[4-[(5-benzyl-1,2,4-oxadiazol-3-yl)carbamoyl]phenyl]cyclohexyl)acetic acid
-
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(trans-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl]cyclohexyl)acetic acid
-
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1-O-Hexadecyl-2-oleoyl-sn-glycerol
-
competitive
3-oxoolean-12-en-27-oic acid
-
the compound exhibits strong inhibition efficacy towards diacylglycerol acyltransferases 1 and 2, and acts competitively against oleoyl-CoA in vitro
3alpha-hydroxyolean-12-en-27-oic acid
-
-
3beta-hydroxyolean-12-en-27-oic acid
-
-
4-[(4-chloro-3-fluorophenyl)methyl]-N-[2-(3,4-diethoxyphenyl)ethyl]-4H-thieno[3,2-b]pyrrole-5-carboxamide
-
EC value is 0.000009 mM
7beta-(3-ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone
-
-
8-angeloyloxy-3,4-epoxy-bisabola-7(14),10-dien-2-one
-
-
aceriphyllic acid A
-
the compound exhibits strong inhibition efficacy towards diacylglycerol acyltransferases 1 and 2, and acts competitively against oleoyl-CoA in vitro
amidepsine A
-
amidepsine B
-
amidepsine C
-
-
amidepsine D
-
betulinic acid
-
a lupane-type triterpenoid, isolated from methanolic extracts of Alnus hirsuta, inhibition of Hep-G2 cell triacyglycerol biosynthesis
cis-4-(4-[[5-(cyclopentylamino)-1,3,4-thiadiazol-2-yl]carbamoyl]phenoxy)cyclohexane-1-carboxylic acid
-
-
cis-4-([5-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]pyridin-2-yl]oxy)cyclohexane-1-carboxylic acid
-
-
cis-4-[4-([3-[(3,5-difluorophenyl)methyl]-1,2,4-oxadiazol-5-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
-
-
cis-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
-
-
cis-4-[4-([5-[(cyclopentyloxy)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
-
-
cis-4-[4-[(3-benzyl-1,2,4-oxadiazol-5-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
-
-
cis-4-[4-[(5-anilino-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
-
-
cis-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
-
-
cis-4-[[5-([5-[(3-chlorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)pyridin-2-yl]oxy]cyclohexane-1-carboxylic acid
-
-
DTT
-
above 2 mM
ethyl 1-(1-[[(2-chlorophenyl)carbamoyl]amino]cyclohexane-1-carbonyl)piperidine-4-carboxylate
-
EC value is 0.0015 mM
ethyl 1-[N-[(2,4-dichlorophenyl)carbamoyl]-2-methylalanyl]piperidine-4-carboxylate
-
EC value is 0.00025 mM
gypsogenic acid
-
-
JNJ-DGAT2-A
-
-
JNJ-DGAT2-B
-
-
kurarinone
-
-
methyl 1-benzyl-3-[(furan-3-carbonyl)amino]-5-[(2-methylbutyl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl 1-benzyl-3-[(furan-3-carbonyl)amino]-5-[[(thiophen-3-yl)methyl]amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl 3-benzamido-1-[(furan-2-yl)methyl]-5-[(2-methylbutyl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl 3-[(furan-2-carbonyl)amino]-1-(3-methylbutyl)-5-[(pentan-3-yl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl 3-[(furan-3-carbonyl)amino]-1-(2-methylpropyl)-5-[(pentan-3-yl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl 5-[(2,3-dihydro-1H-inden-2-yl)amino]-3-[(furan-3-carbonyl)amino]-1-(2-methylpropyl)-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl 5-[[(4-acetamidophenyl)methyl]amino]-1-benzyl-3-[(furan-3-carbonyl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl 5-[[(furan-3-yl)methyl]amino]-1-(2-methylpropyl)-3-(2-phenylacetamido)-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
MgCl2
N-(1-[[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]amino]-2-methyl-1-oxopropan-2-yl)-4-fluorobenzamide
-
-
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
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-carbamoylcyclohexyl)benzamide
-
-
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-[[2-(dimethylamino)ethyl]carbamoyl]cyclohexyl)benzamide
-
-
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-[[2-(morpholin-4-yl)ethyl]carbamoyl]cyclohexyl)benzamide
-
-
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2,3-dihydroxypropyl)carbamoyl]cyclohexyl]benzamide
-
-
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2-hydroxy-2-methylpropyl)carbamoyl]cyclohexyl]benzamide
-
-
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2-methoxyethyl)carbamoyl]cyclohexyl]benzamide
-
-
N-[(2S)-1-ethoxy-4-phenylbutan-2-yl]-1-[2-(tricyclo[3.3.1.1~3,7~]decan-2-yl)acetamido]cyclopentane-1-carboxamide
-
-
N-[1,5-bis(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
-
-
N-[1-(3,5-dimethylphenyl)-4,5,6,7-tetrahydro-1H-indazol-4-yl]-1,2,3-thiadiazole-4-carboxamide
-
EC value is 0.10 mM
N-[1-(4-fluoro-2-methylphenyl)-5-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
-
-
N-[1-(4-fluorophenyl)-5-[2-(4-fluorophenyl)propan-2-yl]-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
-
-
N-[1-(4-hydroxyphenyl)-4,5,6,7-tetrahydro-1H-indazol-4-yl]pyridine-2-carboxamide
-
EC value is 0.00000034 mM
N-[2-(3,4-diethoxyphenyl)ethyl]-4-methyl-4H-thieno[3,2-b]pyrrole-5-carboxamide
-
EC value is 0.011 mM
N-[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-(1-methylcyclopropane-1-carbonyl)alaninamide
-
-
N-[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
-
-
oleanolic acid
-
-
oleate
-
noncompetitive inhibition, IC50: 0.0545 mM
P-7435
-
-
pradigastat
-
-
roselipin 1a
-
roselipin 1B
-
roselipin 2A
-
roselipin 2B
-
tert-butyl (2S)-2-[[1-([(2S)-2-[(2,2-dimethylpropanoyl)oxy]-4-methylpentanoyl]amino)cyclopentane-1-carbonyl]amino]-4-phenylbutanoate
-
-
trans-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
-
-
trans-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
-
-
tussilagone
-
-
tussilagonone
-
-
XP620
[trans-4-(4-[[5-(2-cyclopentylethyl)-1,3,4-thiadiazol-2-yl]carbamoyl]phenyl)cyclohexyl]acetic acid
-
-
[trans-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
-
-
[trans-4-[4-([5-[(4-fluorophenyl)methyl]-1,3,4-oxadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
-
-
[trans-4-[4-([5-[(4-fluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
-
-
[trans-4-[4-([5-[(cyclopentyloxy)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
-
-
[trans-4-[4-([5-[2-(oxolan-2-yl)ethyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
-
-
[trans-4-[4-([5-[2-(oxolan-3-yl)ethyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
-
-
additional information
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.032
1-O-Hexadecyl-2-oleoyl-sn-glycerol
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000326
(4-[4-[4-(2-amino-5-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
Homo sapiens
pH 7.4, 25°C, recombinant enzyme in microsomes of Spodoptera frugiperda cells
0.000276
(4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
Homo sapiens
pH 7.4, 25°C, recombinant enzyme in microsomes of Spodoptera frugiperda cells
0.001
(4-[4-[4-(5-chloro-2-nitrobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
Homo sapiens
above, pH 7.4, 25°C
0.000351
(4-[4-[4-([[2-fluoro-5-(trifluoromethyl)phenyl]carbamoyl]amino)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
Homo sapiens
pH 7.4, 25°C, recombinant enzyme in microsomes of Spodoptera frugiperda cells
0.00046
(4S,7R)-4-(5,5-dimethyl-4-oxo-4,5-dihydrofuran-2-yl)-2,2-dimethyl-4,7-bis[(4E)-4-methyl-5-[(2R)-4-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl]pent-4-en-1-yl]-4,5,6,7-tetrahydro-1-benzofuran-3(2H)-one
Homo sapiens
pH 7.4, temperature not specified in the publication
0.000409
3-(4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)propanoic acid
Homo sapiens
pH 7.4, 25°C, recombinant enzyme in microsomes of Spodoptera frugiperda cells
0.001
4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexane-1-carboxylic acid
Homo sapiens
above, pH 7.4, 25°C
0.04
amidepsine A
Homo sapiens
-
0.03
amidepsine B
Homo sapiens
-
0.2
amidepsine C
Homo sapiens
-
-
0.02
amidepsine D
Homo sapiens
-
0.0708
N-(4,5-dihydronaphtho[1,2-d]thiazol-2-yl)-2-(3,4-dimethoxy phenyl)acetamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.04
xanthohumol
Homo sapiens
-
0.000019
[(1r,4r)-4-[4-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]cyclohexyl]acetic acid
Homo sapiens
pH 7.4, temperature not specified in the publication
0.000157
[(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
Homo sapiens
pH 7.4, 25°C
0.00008
[(1r,4r)-4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl]acetic acid
Homo sapiens
pH 7.4, temperature not specified in the publication
0.000398
[4-(4-[4-[(naphthalene-2-carbonyl)amino]phenyl]thieno[3,2-d]pyrimidin-7-yl)cyclohexyl]acetic acid
Homo sapiens
pH 7.4, 25°C, recombinant enzyme in microsomes of Spodoptera frugiperda cells
0.000121
[4-[4-(4-[[(3-chlorophenyl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
Homo sapiens
pH 7.4, 25°C, recombinant enzyme in microsomes of Spodoptera frugiperda cells
1
[4-[4-(4-[[(4-chloropyridin-2-yl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
Homo sapiens
above, pH 7.4, 25°C
1
[4-[4-(4-[[(5-bromopyridin-3-yl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
Homo sapiens
above, pH 7.4, 25°C
0.000152
[4-[4-(4-[[2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carbonyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
Homo sapiens
pH 7.4, 25°C, recombinant enzyme in microsomes of Spodoptera frugiperda cells
0.001
[4-[4-(4-[[6-(trifluoromethyl)pyridine-3-carbonyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
Homo sapiens
above, pH 7.4, 25°C
0.01
(2S)-1-(3-[[(2S)-1-ethoxy-4-phenylbutan-2-yl]sulfamoyl]anilino)-4-methyl-1-oxopentan-2-yl 2,2-dimethylpropanoate
Homo sapiens
-
IC50 less than 0.01 mM, at pH 7.5 and 25°C
0.000011
(2S)-1-[(1-[[(1S)-1-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-3-phenylpropyl]carbamoyl]cyclopentyl)amino]-4-methyl-1-oxopentan-2-yl 2,2-dimethylpropanoate
Homo sapiens
-
at pH 7.5 and 25°C
0.00036
(trans-4-(4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
Homo sapiens
-
pH not specified in the publication, 25°C
0.000019
(trans-4-(4-[(5-cyclopentylethyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
Homo sapiens
-
pH not specified in the publication, 25°C
0.000024
(trans-4-(4-[(5-cyclopentylmethyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
Homo sapiens
-
pH not specified in the publication, 25°C
0.000045
(trans-4-(4-[(5-[1-fluorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
Homo sapiens
-
pH not specified in the publication, 25°C
0.00003
(trans-4-(4-[(5-[2-chlorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
Homo sapiens
-
pH not specified in the publication, 25°C
0.00003
(trans-4-(4-[(5-[2-fluorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
Homo sapiens
-
pH not specified in the publication, 25°C
0.000253
(trans-4-[4-[(3-benzyl-1,2,4-oxadiazol-5-yl)carbamoyl]phenyl]cyclohexyl)acetic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.000286
(trans-4-[4-[(5-benzyl-1,2,4-oxadiazol-3-yl)carbamoyl]phenyl]cyclohexyl)acetic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.000036
(trans-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl]cyclohexyl)acetic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.1607
7beta-(3-ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone
Homo sapiens
-
-
0.2944
8-angeloyloxy-3,4-epoxy-bisabola-7(14),10-dien-2-one
Homo sapiens
-
-
0.07
amidepsine A
Homo sapiens
-
0.06
amidepsine B
Homo sapiens
-
0.03
amidepsine D
Homo sapiens
-
0.000022
cis-4-(4-[[5-(cyclopentylamino)-1,3,4-thiadiazol-2-yl]carbamoyl]phenoxy)cyclohexane-1-carboxylic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.000045
cis-4-([5-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]pyridin-2-yl]oxy)cyclohexane-1-carboxylic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.00012
cis-4-[4-([3-[(3,5-difluorophenyl)methyl]-1,2,4-oxadiazol-5-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.000011
cis-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.000012
cis-4-[4-([5-[(cyclopentyloxy)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.000057
cis-4-[4-[(3-benzyl-1,2,4-oxadiazol-5-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.000004
cis-4-[4-[(5-anilino-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.000016
cis-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.000055
cis-4-[[5-([5-[(3-chlorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)pyridin-2-yl]oxy]cyclohexane-1-carboxylic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.0288
kurarinone
Homo sapiens
-
-
0.0059
methyl 1-benzyl-3-[(furan-3-carbonyl)amino]-5-[(2-methylbutyl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
Homo sapiens
-
at pH 7.4 and 37°C
0.0082
methyl 1-benzyl-3-[(furan-3-carbonyl)amino]-5-[[(thiophen-3-yl)methyl]amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
Homo sapiens
-
at pH 7.4 and 37°C
0.0074
methyl 3-benzamido-1-[(furan-2-yl)methyl]-5-[(2-methylbutyl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
Homo sapiens
-
at pH 7.4 and 37°C
0.0091
methyl 3-[(furan-2-carbonyl)amino]-1-(3-methylbutyl)-5-[(pentan-3-yl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
Homo sapiens
-
at pH 7.4 and 37°C
0.0088
methyl 3-[(furan-3-carbonyl)amino]-1-(2-methylpropyl)-5-[(pentan-3-yl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
Homo sapiens
-
at pH 7.4 and 37°C
0.0072
methyl 5-[(2,3-dihydro-1H-inden-2-yl)amino]-3-[(furan-3-carbonyl)amino]-1-(2-methylpropyl)-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
Homo sapiens
-
at pH 7.4 and 37°C
0.0295
methyl 5-[[(4-acetamidophenyl)methyl]amino]-1-benzyl-3-[(furan-3-carbonyl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
Homo sapiens
-
at pH 7.4 and 37°C
0.0192
methyl 5-[[(furan-3-yl)methyl]amino]-1-(2-methylpropyl)-3-(2-phenylacetamido)-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
Homo sapiens
-
at pH 7.4 and 37°C
0.0035
N-(1-[[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]amino]-2-methyl-1-oxopropan-2-yl)-4-fluorobenzamide
Homo sapiens
-
at pH 7.5 and 25°C
0.0085
N-(4,5-dihydronaphtho[1,2-d]thiazol-2-yl)-2-(3,4-dimethoxy phenyl)acetamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000048
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-carbamoylcyclohexyl)benzamide
Homo sapiens
-
at pH 7.4 and 37°C
0.000279
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-[[2-(dimethylamino)ethyl]carbamoyl]cyclohexyl)benzamide
Homo sapiens
-
at pH 7.4 and 37°C
0.000122
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-[[2-(morpholin-4-yl)ethyl]carbamoyl]cyclohexyl)benzamide
Homo sapiens
-
at pH 7.4 and 37°C
0.000081
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2,3-dihydroxypropyl)carbamoyl]cyclohexyl]benzamide
Homo sapiens
-
at pH 7.4 and 37°C
0.000092
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2-hydroxy-2-methylpropyl)carbamoyl]cyclohexyl]benzamide
Homo sapiens
-
at pH 7.4 and 37°C
0.000088
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2-methoxyethyl)carbamoyl]cyclohexyl]benzamide
Homo sapiens
-
at pH 7.4 and 37°C
0.000027
N-[(2S)-1-ethoxy-4-phenylbutan-2-yl]-1-[2-(tricyclo[3.3.1.1~3,7~]decan-2-yl)acetamido]cyclopentane-1-carboxamide
Homo sapiens
-
at pH 7.5 and 25°C
0.00076
N-[1,5-bis(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
Homo sapiens
-
at pH 7.5 and 25°C
0.000062
N-[1-(4-fluoro-2-methylphenyl)-5-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
Homo sapiens
-
at pH 7.5 and 25°C
0.0014
N-[1-(4-fluorophenyl)-5-[2-(4-fluorophenyl)propan-2-yl]-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
Homo sapiens
-
at pH 7.5 and 25°C
0.01
N-[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-(1-methylcyclopropane-1-carbonyl)alaninamide
Homo sapiens
-
IC50 less than 0.01 mM, at pH 7.5 and 25°C
0.0048
N-[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
Homo sapiens
-
at pH 7.5 and 25°C
0.0545
oleate
Homo sapiens
-
noncompetitive inhibition, IC50: 0.0545 mM
0.03
roselipin 1a
Homo sapiens
-
0.04
roselipin 1B
Homo sapiens
-
0.045
roselipin 2A
Homo sapiens
-
0.05
roselipin 2B
Homo sapiens
-
0.000007
tert-butyl (2S)-2-[[1-([(2S)-2-[(2,2-dimethylpropanoyl)oxy]-4-methylpentanoyl]amino)cyclopentane-1-carbonyl]amino]-4-phenylbutanoate
Homo sapiens
-
at pH 7.5 and 25°C
0.00016
trans-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.00028
trans-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.0491
tussilagone
Homo sapiens
-
-
0.04
xanthohumol
Homo sapiens
-
0.0000166 - 0.001499
XP620
0.000019
[trans-4-(4-[[5-(2-cyclopentylethyl)-1,3,4-thiadiazol-2-yl]carbamoyl]phenyl)cyclohexyl]acetic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.000009
[trans-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.00139
[trans-4-[4-([5-[(4-fluorophenyl)methyl]-1,3,4-oxadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.0006
[trans-4-[4-([5-[(4-fluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.000038
[trans-4-[4-([5-[(cyclopentyloxy)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.000144
[trans-4-[4-([5-[2-(oxolan-2-yl)ethyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
Homo sapiens
-
at pH 7.4 and 37°C
0.000233
[trans-4-[4-([5-[2-(oxolan-3-yl)ethyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
Homo sapiens
-
at pH 7.4 and 37°C
additional information
roselipin 1a
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.0035 - 0.0134
-
transfected cells
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.1
-
broad
7.4
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
25
assay at
25
-
assay at
additional information
-
assay at various temperatures from 24°C to 40°C
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
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
malfunction
-
phenotypic analysis of thienopyrrole (CT2) inhibitor treated cells, overview
physiological function
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
DGAT1_HUMAN
488
9
55278
Swiss-Prot
other Location (Reliability: 5)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
150000
-
gel filtration
42000
-
2 * 42000, SDS-PAGE
50000
90000
-
gel filtration, the enzyme is part of large 650000 Da protein complex
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
-
x * 50000, SDS-PAGE
homodimer
-
2 * 42000, SDS-PAGE
tetramer
-
4 * 50000, SDS-PAGE
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
25
-
labile above, gradual inactivation
40
-
20% loss of activity after 15 min
50
-
t1/2: 15 min
65
-
inactivation after 15 min
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-20°C, 30 days, microsomal preparation
-
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
recombinant enzyme DGAT in Spodoptera frugiperda Sf9 cell microsomes
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expressed in Saccharomyces cerevisiae
expression in baculoviral system
gene DGAT1, recombinant expression of the isozyme in Spodoptera frugiperda Sf9 cells via baculovirus transfection method
chromosomal location, expression of the FLAG-tagged enzyme in Spodoptera frugiperda Sf9 cells and in COS-7 cells
-
DGATsv, splice variant, deletion of 101 residues from the C-terminus, enzymatically inactive
-
expressed in a baculovirus expression system
-
expressed in HEK-293T cells, RH-7777 cells, and COS-7 cells
-
expressed in Saccharomyces cerevisiae
expressed in Sf9 insect cells
-
expression in baculoviral system
expression in Sf9 cell
-
gene DC3, location of DC3 on the X chromosome at Xq13.1, DNA and amino acid sequence determination and analysis, expression analysis, expression in Saccharomyces cerevisiae
gene DGAT2, localization of DGAT2 at 11q13.5, DNA and amino acid sequence determination and analysis, expression analysis, expression in Saccharomyces cerevisiae
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
diacylglycerol acyltransferase (DGAT), the only limited enzyme in the synthesis of triacylglycerol (TAG), is regarded as an important therapeutic target for human obesity and other metabolic syndromes
drug development
-
the enzyme is a target for development of inhibitors of lipid deposition
medicine
-
enzyme expression is decreased in psoriatic skin
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Kawasaki, T.; Snyder, F.
Synthesis of a novel acetylated neutral lipid related to platelet-activating factor by acyl-CoA:1-O-alkyl-2-acetyl-sn-glycerol acyltransferase in HL-60 cells [published erratum appears in J Biol Chem 1988 Jul 25;263(21):10539]
J. Biol. Chem.
263
2593-2596
1988
Homo sapiens
Manually annotated by BRENDA team
Cases, S.; Smith, S.J.; Zheng, Y.W.; Myers, H.M.; Lear, S.R.; Sande, E.; Novak, S.; Collins, C.; Welch, C.B.; Lusis, A.J.; Erickson, S.K.; Farese, R.V., Jr.
Identification of a gene encoding an acyl CoA:diacylglycerol acyltransferase, a key enzyme in triacylglycerol synthesis
Proc. Natl. Acad. Sci. USA
95
13018-13023
1998
Homo sapiens, Mus musculus (Q9Z2A7), Mus musculus
Manually annotated by BRENDA team
Cases, S.; Stone, S.J.; Zhou, P.; Yen, E.; Tow, B.; Lardizabal, K.D.; Voelker, T.; Farese, R.V., Jr.
Cloning of DGAT2, a second mammalian diacylglycerol acyltransferase, and related family members
J. Biol. Chem.
276
38870-38876
2001
Homo sapiens (Q96PD7), Homo sapiens, Mus musculus (Q9DCV3), Mus musculus
Manually annotated by BRENDA team
Cheng, D.; Meegalla, R.L.; He, B.; Cromley, D.A.; Billheimer, J.T.; Young, P.R.
Human acyl-CoA:diacylglycerol acyltransferase is a tetrameric protein
Biochem. J.
359
707-714
2001
Homo sapiens
Manually annotated by BRENDA team
Wakimoto, K.; Chiba, H.; Michibata, H.; Seishima, M.; Kawasaki, S.; Okubo, K.; Mitsui, H.; Torii, H.; Imai, Y.
A novel diacylglycerol acyltransferase (DGAT2) is decreased in human psoriatic skin and increased in diabetic mice
Biochem. Biophys. Res. Commun.
310
296-302
2003
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
Turkish, A.R.; Henneberry, A.L.; Cromley, D.; Padamsee, M.; Oelkers, P.; Bazzi, H.; Christiano, A.M.; Billheimer, J.T.; Sturley, S.L.
Identification of two novel human acyl-CoA wax alcohol acyltransferases: members of the diacylglycerol acyltransferase 2 (DGAT2) gene superfamily
J. Biol. Chem.
280
14755-14764
2005
Homo sapiens, Homo sapiens (Q6ZPD8), Homo sapiens (Q96PD7)
Manually annotated by BRENDA team
Chung, M.Y.; Rho, M.C.; Lee, S.W.; Park, H.R.; Kim, K.; Lee, I.A.; Kim, D.H.; Jeune, K.H.; Lee, H.S.; Kim, Y.K.
Inhibition of diacylglycerol acyltransferase by betulinic acid from Alnus hirsuta
Planta Med.
72
267-269
2006
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Park, H.R.; Yoo, M.Y.; Seo, J.H.; Kim, I.S.; Kim, N.Y.; Kang, J.Y.; Cui, L.; Lee, C.S.; Lee, C.H.; Lee, H.S.
Sesquiterpenoids isolated from the flower buds of Tussilago farfara L. inhibit diacylglycerol acyltransferase
J. Agric. Food Chem.
56
10493-10497
2008
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Inokoshi, J.; Kawamoto, K.; Takagi, Y.; Matsuhama, M.; Omura, S.; Tomoda, H.
Expression of two human acyl-CoA:diacylglycerol acyltransferase isozymes in yeast and selectivity of microbial inhibitors toward the isozymes
J. Antibiot.
62
51-54
2009
Homo sapiens (O75907), Homo sapiens (Q96PD7), Homo sapiens
Manually annotated by BRENDA team
Cheng, D.; Iqbal, J.; Devenny, J.; Chu, C.H.; Chen, L.; Dong, J.; Seethala, R.; Keim, W.J.; Azzara, A.V.; Lawrence, R.M.; Pelleymounter, M.A.; Hussain, M.M.
Acylation of acylglycerols by acyl coenzyme A:diacylglycerol acyltransferase 1 (DGAT1). Functional importance of DGAT1 in the intestinal fat absorption
J. Biol. Chem.
283
29802-29811
2008
Homo sapiens, Mus musculus, Rattus norvegicus
Manually annotated by BRENDA team
Hou, X.G.; Moser, S.; Sarr, M.G.; Thompson, G.B.; Que, F.G.; Jensen, M.D.
Visceral and subcutaneous adipose tissue diacylglycerol acyltransferase activity in humans
Obesity (Silver Spring)
17
1129-1134
2009
Homo sapiens
Manually annotated by BRENDA team
Mougenot, P.; Namane, C.; Fett, E.; Camy, F.; Dadji-Faihun, R.; Langot, G.; Monseau, C.; Onofri, B.; Pacquet, F.; Pascal, C.; Crespin, O.; Ben-Hassine, M.; Ragot, J.L.; Van-Pham, T.; Philippo, C.; Chatelain-Egger, F.; Peron, P.; Le Bail, J.C.; Guillot, E.; Chamiot-Clerc, P.; Chabanaud, M.A.; Pruniaux, M.-P.; Schmidt, F.; Venier, O.; Nicolai, E.; Viviani, F.
Thiadiazoles as new inhibitors of diacylglycerol acyltransferase type 1
Bioorg. Med. Chem. Lett.
22
2497-2502
2012
Homo sapiens
Manually annotated by BRENDA team
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
FEBS J.
279
3033-3047
2012
Homo sapiens (O75907), Homo sapiens (Q96PD7), Homo sapiens
Manually annotated by BRENDA team
Hiramine, Y.; Tanabe, T.
Characterization of acyl-coenzyme A:diacylglycerol acyltransferase (DGAT) enzyme of human small intestine
J. Physiol. Biochem.
67
259-264
2011
Homo sapiens
Manually annotated by BRENDA team
Kim, M.O.; Lee, S.; Choi, K.; Lee, S.; Kim, H.; Kang, H.; Choi, M.; Kwon, E.B.; Kang, M.J.; Kim, S.; Lee, H.J.; Lee, H.S.; Kwak, Y.S.; Cho, S.
Discovery of a novel class of diacylglycerol acyltransferase 2 inhibitors with a 1H-pyrrolo[2,3-b]pyridine core
Biol. Pharm. Bull.
37
1655-1660
2014
Homo sapiens
Manually annotated by BRENDA team
Nakajima, K.; April, M.; Brewer, J.T.; Daniels, T.; Forster, C.J.; Gilmore, T.A.; Jain, M.; Kanter, A.; Kwak, Y.; Li, J.; McQuire, L.; Serrano-Wu, M.H.; Streeper, R.; Szklennik, P.; Thompson, J.; Wang, B.
Discovery of diamide compounds as diacylglycerol acyltransferase 1 (DGAT1) inhibitors
Bioorg. Med. Chem. Lett.
26
1245-1248
2016
Homo sapiens
Manually annotated by BRENDA team
Mougenot, P.; Namane, C.; Fett, E.; Goumy, F.; Dadji-Faihun, R.; Langot, G.; Monseau, C.; Onofri, B.; Pacquet, F.; Pascal, C.; Crespin, O.; Ben-Hassine, M.; Ragot, J.L.; Van-Pham, T.; Philippo, C.; Chatelain-Egger, F.; Peron, P.; Le Bail, J.C.; Guillot, E.; Chamiot-Clerc, P.; Chabanaud, M.A.; Pruniaux, M.-P.
Synthesis and multiparametric evaluation of thiadiazoles and oxadiazoles as diacylglycerol acyltransferase type 1 inhibitors
Bioorg. Med. Chem. Lett.
26
25-32
2016
Homo sapiens
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
Seo, J.H.; Kim, M.O.; Han, A.R.; Kwon, E.B.; Kang, M.J.; Cho, S.; Moon, D.O.; Noh, J.R.; Lee, C.H.; Kim, Y.S.; Lee, H.S.
Oleanane-type triterpenoids of Aceriphyllum rossii and their diacylglycerol acyltransferase-inhibitory activity
Planta Med.
81
228-234
2015
Homo sapiens
Manually annotated by BRENDA team
Li, D.; Yin, J.; Li, J.; Nan, F.
Design and synthesis of diacylglycerol acyltransferase 1 inhibitors based on Aphadilactone C
Chinese J. Org. Chem.
36
1359-1367
2016
Homo sapiens (O75907)
-
Manually annotated by BRENDA team
Tschapalda, K.; Zhang, Y.Q.; Liu, L.; Golovnina, K.; Schlemper, T.; Eichmann, T.O.; Lal-Nag, M.; Sreenivasan, U.; McLenithan, J.; Ziegler, S.; Sztalryd, C.; Lass, A.; Auld, D.; Oliver, B.; Waldmann, H.; Li, Z.; Shen, M.; Boxer, M.B.; Beller, M.
A class of diacylglycerol acyltransferase 1 inhibitors identified by a combination of phenotypic high-throughput screening, genomics, and genetics
EBioMedicine
8
49-59
2016
Homo sapiens
Manually annotated by BRENDA team
Hong, D.J.; Jung, S.H.; Kim, J.; Jung, D.; Ahn, Y.G.; Suh, K.H.; Min, K.H.
Synthesis and biological evaluation of novel thienopyrimidine derivatives as diacylglycerol acyltransferase 1 (DGAT-1) inhibitors
J. Enzyme Inhib. Med. Chem.
35
227-234
2020
Canis lupus familiaris (E2RDN4), Canis lupus familiaris, Homo sapiens (O75907), Rattus norvegicus (Q9ERM3), Mus musculus (Q9Z2A7), Mus musculus
Manually annotated by BRENDA team
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