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Literature summary extracted from

  • 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 (2016), EBioMedicine, 8, 49-59 .
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.3.1.20 drug development the enzyme is a target for development of inhibitors of lipid deposition Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.20 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 Homo sapiens
2.3.1.20 ethyl 1-(1-[[(2-chlorophenyl)carbamoyl]amino]cyclohexane-1-carbonyl)piperidine-4-carboxylate EC value is 0.0015 mM Homo sapiens
2.3.1.20 ethyl 1-[N-[(2,4-dichlorophenyl)carbamoyl]-2-methylalanyl]piperidine-4-carboxylate EC value is 0.00025 mM Homo sapiens
2.3.1.20 additional information high-throughput screening for enzyme inhibitors, quantitative-high throughput image-based assay, overview. The activity of the identified lipid storage inhibitors is evolutionary conserved. Three scaffolds: structures are characterized by a tetrahydroindazole (CT1), thienopyrrole (CT2) or arylureido (CT3) core, phenotypic analysis of thienopyrrole (CT2) treated cells Homo sapiens
2.3.1.20 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 Homo sapiens
2.3.1.20 N-[1-(4-hydroxyphenyl)-4,5,6,7-tetrahydro-1H-indazol-4-yl]pyridine-2-carboxamide EC value is 0.00000034 mM Homo sapiens
2.3.1.20 N-[2-(3,4-diethoxyphenyl)ethyl]-4-methyl-4H-thieno[3,2-b]pyrrole-5-carboxamide EC value is 0.011 mM Homo sapiens

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 Homo sapiens
-
CoA + 1,2,3-triacylglycerol
-
?

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.20 Homo sapiens
-
-
-

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
-
Homo sapiens CoA + 1,2,3-triacylglycerol
-
?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.20 DGAT1
-
Homo sapiens
2.3.1.20 diacylglycerol acyltransferase 1
-
Homo sapiens

General Information

EC Number General Information Comment Organism
2.3.1.20 malfunction phenotypic analysis of thienopyrrole (CT2) inhibitor treated cells, overview Homo sapiens
2.3.1.20 physiological function diacylglycerol acyltransferase 1 (DGAT1) is a key enzyme in the production of triacylglycerols Homo sapiens