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Literature summary for 3.4.14.5 extracted from

  • Zhu, L.; Li, Y.; Qiu, L.; Su, M.; Wang, X.; Xia, C.; Qu, Y.; Li, J.; Li, J.; Xiong, B.; Shen, J.
    Design and synthesis of 4-(2,4,5-trifluorophenyl)butane-1,3-diamines as dipeptidyl peptidase IV inhibitors (2013), ChemMedChem, 8, 1104-1116.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitor N-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butyl]-6-(trifluoromethyl)-3,4-dihydropyrrolo[1,2-a]pyrazine-2(1H)-carboxamide, to 3.2 A resolution Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
N-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butyl]-6-(trifluoromethyl)-3,4-dihydropyrrolo[1,2-a]pyrazine-2(1H)-carboxamide good enzyme inhibitory activity and excellent selectivity for isoform DPP4 over dipeptidyl peptidase family homologues DPP8 and DPP9. Compound shows efficacy similar to that of sitagliptin in the oral glucose tolerance test Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
104400
-
x * 104400, mass spectrometry, x * 110000, SDS-PAGE Homo sapiens
110000
-
x * 104400, mass spectrometry, x * 110000, SDS-PAGE Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
glycoprotein glycosylation can be estimated to account for 24% of the molecular mass of the whole glycosylated protein Homo sapiens

Subunits

Subunits Comment Organism
? x * 104400, mass spectrometry, x * 110000, SDS-PAGE Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000031
-
pH 7.5, temperature not specified in the publication Homo sapiens N-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butyl]-6-(trifluoromethyl)-3,4-dihydropyrrolo[1,2-a]pyrazine-2(1H)-carboxamide