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Literature summary for 2.3.1.20 extracted from

  • 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 (2020), J. Enzyme Inhib. Med. Chem., 35, 227-234 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.3.1.20

Cloned(Commentary)

Cloned (Comment) Organism
gene DGAT1, recombinant expression of the isozyme in Spodoptera frugiperda Sf9 cells via baculovirus transfection method Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(1R,2R)-2-[4'-[(phenylcarbamoyl)amino][1,1'-biphenyl]-4-carbonyl]cyclopentane-1-carboxylic acid
-
 Homo sapiens
(4-[4-[4-(2-amino-5-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
 Homo sapiens
(4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
 Homo sapiens
(4-[4-[4-(5-chloro-2-nitrobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
 Homo sapiens
(4-[4-[4-([[2-fluoro-5-(trifluoromethyl)phenyl]carbamoyl]amino)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
 Homo sapiens
3-(4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)propanoic acid
-
 Homo sapiens
4-[4-(4-[[2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carbonyl]amino]phenyl)piperidine-1-carbonyl]cyclohexane-1-carboxylic acid
-
 Homo sapiens
4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexane-1-carboxylic acid
-
 Homo sapiens
cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
 Canis lupus familiaris
cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
 Homo sapiens
cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
 Mus musculus
cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
 Rattus norvegicus
cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetic acid
-
 Homo sapiens
methyl 2-(4-(4-(4-((tert-butoxycarbonyl)amino)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohex-3-en-1-yl)acetate
-
 Homo sapiens
methyl 2-(4-(4-(4-((tert-butoxycarbonyl)amino)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl) acetate
-
 Homo sapiens
methyl 2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
 Homo sapiens
methyl 2-(4-(4-(4-aminophenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
 Homo sapiens
methyl cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
 Homo sapiens
methyl trans-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
 Homo sapiens
additional information in vivo inhibitory activity thieno[3,2-d]pyrimidine derivatives against diacylglycerol acyltransferase 1 (DGAT-1) and effects on microsomes and cytochrome P-450, overview Canis lupus familiaris
additional information a series of thieno[3,2-d]pyrimidine derivatives are synthesized and their inhibitory effects against diacylglycerol acyltransferase 1 (DGAT-1) are assessed Homo sapiens
additional information in vivo inhibitory activity thieno[3,2-d]pyrimidine derivatives against diacylglycerol acyltransferase 1 (DGAT-1) and effects on microsomes and cytochrome P-450, overview Mus musculus
additional information in vivo inhibitory activity thieno[3,2-d]pyrimidine derivatives against diacylglycerol acyltransferase 1 (DGAT-1) and effects on microsomes and cytochrome P-450, overview Rattus norvegicus
tert-butyl (4-(7-bromothieno[3,2-d]pyrimidin-4-yl)phenyl)carbamate
-
 Homo sapiens
trans-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
 Homo sapiens
trans-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetic acid
-
 Homo sapiens
[(1r,4r)-4-(4-[[5-(3,4-difluoroanilino)-1,3,4-oxadiazole-2-carbonyl]amino]phenyl)cyclohexyl]acetic acid
-
 Homo sapiens
[(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
[(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
-
 Canis lupus familiaris
[(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
-
 Homo sapiens
[(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
-
 Mus musculus
[(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
-
 Rattus norvegicus
[4-(4-[4-[(naphthalene-2-carbonyl)amino]phenyl]thieno[3,2-d]pyrimidin-7-yl)cyclohexyl]acetic acid
-
 Homo sapiens
[4-[4-(4-[[(3-chlorophenyl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
 Homo sapiens
[4-[4-(4-[[(4-chloropyridin-2-yl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
 Homo sapiens
[4-[4-(4-[[(5-bromopyridin-3-yl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
 Homo sapiens
[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
[4-[4-(4-[[6-(trifluoromethyl)pyridine-3-carbonyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
 Mus musculus 16020
-
membrane
-
 Homo sapiens 16020
-
membrane
-
 Canis lupus familiaris 16020
-
membrane
-
 Rattus norvegicus 16020
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Mus musculus
Mg2+ required Homo sapiens
Mg2+ required Canis lupus familiaris
Mg2+ required Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
acyl-CoA + 1,2-diacyl-sn-glycerol Mus musculus
-
 CoA + 1,2,3-triacylglycerol
-
 ?
acyl-CoA + 1,2-diacyl-sn-glycerol Homo sapiens
-
 CoA + 1,2,3-triacylglycerol
-
 ?
acyl-CoA + 1,2-diacyl-sn-glycerol Canis lupus familiaris
-
 CoA + 1,2,3-triacylglycerol
-
 ?
acyl-CoA + 1,2-diacyl-sn-glycerol Rattus norvegicus
-
 CoA + 1,2,3-triacylglycerol
-
 ?

Organism

Organism UniProt Comment Textmining
Canis lupus familiaris E2RDN4
-
-
Homo sapiens O75907
-
-
Mus musculus Q9Z2A7
-
-
Rattus norvegicus Q9ERM3
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant enzyme DGAT in Spodoptera frugiperda Sf9 cell microsomes Homo sapiens
wild-type enzyme DGAT in microsomes Mus musculus
wild-type enzyme DGAT in microsomes Canis lupus familiaris
wild-type enzyme DGAT in microsomes Rattus norvegicus

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
 Mus musculus
-
brain
-
 Mus musculus
-
kidney
-
 Mus musculus
-
large intestine
-
 Mus musculus
-
liver
-
 Mus musculus
-
small intestine
-
 Mus musculus
-
spleen
-
 Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acyl-CoA + 1,2-diacyl-sn-glycerol
-
 Mus musculus CoA + 1,2,3-triacylglycerol
-
 ?
acyl-CoA + 1,2-diacyl-sn-glycerol
-
 Homo sapiens CoA + 1,2,3-triacylglycerol
-
 ?
acyl-CoA + 1,2-diacyl-sn-glycerol
-
 Canis lupus familiaris CoA + 1,2,3-triacylglycerol
-
 ?
acyl-CoA + 1,2-diacyl-sn-glycerol
-
 Rattus norvegicus CoA + 1,2,3-triacylglycerol
-
 ?

Synonyms

Synonyms Comment Organism
DGAT-1
-
 Mus musculus
DGAT-1
-
 Homo sapiens
DGAT-1
-
 Canis lupus familiaris
DGAT-1
-
 Rattus norvegicus
DGAT1
-
 Mus musculus
DGAT1
-
 Homo sapiens
DGAT1
-
 Canis lupus familiaris
DGAT1
-
 Rattus norvegicus
diacylglycerol acyltransferase 1
-
 Mus musculus
diacylglycerol acyltransferase 1
-
 Homo sapiens
diacylglycerol acyltransferase 1
-
 Canis lupus familiaris
diacylglycerol acyltransferase 1
-
 Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
 assay at Mus musculus
25
-
 assay at Homo sapiens
25
-
 assay at Canis lupus familiaris
25
-
 assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Mus musculus
7.4
-
 assay at Homo sapiens
7.4
-
 assay at Canis lupus familiaris
7.4
-
 assay at Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000121
-
 pH 7.4, 25°C, recombinant enzyme in microsomes of Spodoptera frugiperda cells Homo sapiens [4-[4-(4-[[(3-chlorophenyl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
0.000152
-
 pH 7.4, 25°C, recombinant enzyme in microsomes of Spodoptera frugiperda cells Homo sapiens [4-[4-(4-[[2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carbonyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
0.000157
-
 pH 7.4, 25°C Homo sapiens [(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
0.000276
-
 pH 7.4, 25°C, recombinant enzyme in microsomes of Spodoptera frugiperda cells Homo sapiens (4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
0.000326
-
 pH 7.4, 25°C, recombinant enzyme in microsomes of Spodoptera frugiperda cells Homo sapiens (4-[4-[4-(2-amino-5-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
0.000351
-
 pH 7.4, 25°C, recombinant enzyme in microsomes of Spodoptera frugiperda cells Homo sapiens (4-[4-[4-([[2-fluoro-5-(trifluoromethyl)phenyl]carbamoyl]amino)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
0.000398
-
 pH 7.4, 25°C, recombinant enzyme in microsomes of Spodoptera frugiperda cells Homo sapiens [4-(4-[4-[(naphthalene-2-carbonyl)amino]phenyl]thieno[3,2-d]pyrimidin-7-yl)cyclohexyl]acetic acid
0.000409
-
 pH 7.4, 25°C, recombinant enzyme in microsomes of Spodoptera frugiperda cells Homo sapiens 3-(4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)propanoic acid
0.001
-
 above, pH 7.4, 25°C Homo sapiens (4-[4-[4-(5-chloro-2-nitrobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
0.001
-
 above, pH 7.4, 25°C Homo sapiens 4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexane-1-carboxylic acid
0.001
-
 above, pH 7.4, 25°C Homo sapiens [4-[4-(4-[[6-(trifluoromethyl)pyridine-3-carbonyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
1
-
 above, pH 7.4, 25°C Homo sapiens [4-[4-(4-[[(4-chloropyridin-2-yl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
1
-
 above, pH 7.4, 25°C Homo sapiens [4-[4-(4-[[(5-bromopyridin-3-yl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid