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Literature summary 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

Cloned(Commentary)

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.20 (1R,2R)-2-[4'-[(phenylcarbamoyl)amino][1,1'-biphenyl]-4-carbonyl]cyclopentane-1-carboxylic acid
-
Homo sapiens
2.3.1.20 (4-[4-[4-(2-amino-5-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
Homo sapiens
2.3.1.20 (4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
Homo sapiens
2.3.1.20 (4-[4-[4-(5-chloro-2-nitrobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
Homo sapiens
2.3.1.20 (4-[4-[4-([[2-fluoro-5-(trifluoromethyl)phenyl]carbamoyl]amino)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
Homo sapiens
2.3.1.20 3-(4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)propanoic acid
-
Homo sapiens
2.3.1.20 4-[4-(4-[[2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carbonyl]amino]phenyl)piperidine-1-carbonyl]cyclohexane-1-carboxylic acid
-
Homo sapiens
2.3.1.20 4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexane-1-carboxylic acid
-
Homo sapiens
2.3.1.20 cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
Canis lupus familiaris
2.3.1.20 cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
Homo sapiens
2.3.1.20 cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
Mus musculus
2.3.1.20 cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
Rattus norvegicus
2.3.1.20 cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetic acid
-
Homo sapiens
2.3.1.20 methyl 2-(4-(4-(4-((tert-butoxycarbonyl)amino)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohex-3-en-1-yl)acetate
-
Homo sapiens
2.3.1.20 methyl 2-(4-(4-(4-((tert-butoxycarbonyl)amino)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl) acetate
-
Homo sapiens
2.3.1.20 methyl 2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
Homo sapiens
2.3.1.20 methyl 2-(4-(4-(4-aminophenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
Homo sapiens
2.3.1.20 methyl cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
Homo sapiens
2.3.1.20 methyl trans-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
Homo sapiens
2.3.1.20 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
2.3.1.20 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
2.3.1.20 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
2.3.1.20 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
2.3.1.20 tert-butyl (4-(7-bromothieno[3,2-d]pyrimidin-4-yl)phenyl)carbamate
-
Homo sapiens
2.3.1.20 trans-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
Homo sapiens
2.3.1.20 trans-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetic acid
-
Homo sapiens
2.3.1.20 [(1r,4r)-4-(4-[[5-(3,4-difluoroanilino)-1,3,4-oxadiazole-2-carbonyl]amino]phenyl)cyclohexyl]acetic acid
-
Homo sapiens
2.3.1.20 [(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
2.3.1.20 [(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
-
Canis lupus familiaris
2.3.1.20 [(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
-
Homo sapiens
2.3.1.20 [(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
-
Mus musculus
2.3.1.20 [(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
-
Rattus norvegicus
2.3.1.20 [4-(4-[4-[(naphthalene-2-carbonyl)amino]phenyl]thieno[3,2-d]pyrimidin-7-yl)cyclohexyl]acetic acid
-
Homo sapiens
2.3.1.20 [4-[4-(4-[[(3-chlorophenyl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
Homo sapiens
2.3.1.20 [4-[4-(4-[[(4-chloropyridin-2-yl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
Homo sapiens
2.3.1.20 [4-[4-(4-[[(5-bromopyridin-3-yl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
Homo sapiens
2.3.1.20 [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
2.3.1.20 [4-[4-(4-[[6-(trifluoromethyl)pyridine-3-carbonyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
Homo sapiens

Localization

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

Metals/Ions

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

Natural Substrates/ Products (Substrates)

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

Organism

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

Purification (Commentary)

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

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

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

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.3.1.20 25
-
assay at Mus musculus
2.3.1.20 25
-
assay at Homo sapiens
2.3.1.20 25
-
assay at Canis lupus familiaris
2.3.1.20 25
-
assay at Rattus norvegicus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.3.1.20 7.4
-
assay at Mus musculus
2.3.1.20 7.4
-
assay at Homo sapiens
2.3.1.20 7.4
-
assay at Canis lupus familiaris
2.3.1.20 7.4
-
assay at Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.20 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
2.3.1.20 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
2.3.1.20 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
2.3.1.20 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
2.3.1.20 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
2.3.1.20 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
2.3.1.20 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
2.3.1.20 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
2.3.1.20 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
2.3.1.20 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
2.3.1.20 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
2.3.1.20 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
2.3.1.20 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