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Literature summary for 3.4.14.5 extracted from

  • Lee, B.; Shi, L.; Kassel, D.B.; Asakawa, T.; Takeuchi, K.; Christopher, R.J.
    Pharmacokinetic, pharmacodynamic, and efficacy profiles of alogliptin, a novel inhibitor of dipeptidyl peptidase-4, in rats, dogs, and monkeys (2008), Eur. J. Pharmacol., 589, 306-314.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed using baculovirus Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
alogliptin nanomolar inhibitor of DPP-4, i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, exhibits 10000fold selectivity for DPP-4 over the closely related serine proteases DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidase, and tryptase, about 75% inhibition of DPP-4 24 h after treatment with 3 mg/kg alogliptin Canis lupus familiaris
alogliptin nanomolar inhibitor of DPP-4, i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, exhibits 10000fold selectivity for DPP-4 over the closely related serine proteases DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidase, and tryptase Homo sapiens
alogliptin nanomolar inhibitor of DPP-4, i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, exhibits 10000fold selectivity for DPP-4 over the closely related serine proteases DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidase, and tryptase, about 15% inhibition of DPP-4 24 h after treatment with 3 mg/kg alogliptin Macaca fascicularis
alogliptin nanomolar inhibitor of DPP-4, i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, exhibits 10000fold selectivity for DPP-4 over the closely related serine proteases DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidase, and tryptase, complete inhibition of DPP-4 24 h after treatment with 10 mg/kg alogliptin Rattus norvegicus
sitagliptin (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine Canis lupus familiaris
sitagliptin (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine Homo sapiens
sitagliptin (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine Macaca fascicularis
sitagliptin (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine Rattus norvegicus
vildagliptin i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine Canis lupus familiaris
vildagliptin i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine Homo sapiens
vildagliptin i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine Macaca fascicularis
vildagliptin i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Canis lupus familiaris
-
-
-
Homo sapiens
-
-
-
Macaca fascicularis
-
-
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Homo sapiens
-
blood plasma
-
Rattus norvegicus
-
blood plasma
-
Canis lupus familiaris
-
blood plasma
-
Macaca fascicularis
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-Ala-L-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens L-Ala-L-Pro + 7-amino-4-methylcoumarin
-
?
L-Ala-L-Pro-7-amido-4-methylcoumarin + H2O
-
Rattus norvegicus L-Ala-L-Pro + 7-amino-4-methylcoumarin
-
?
L-Ala-L-Pro-7-amido-4-methylcoumarin + H2O
-
Canis lupus familiaris L-Ala-L-Pro + 7-amino-4-methylcoumarin
-
?
L-Ala-L-Pro-7-amido-4-methylcoumarin + H2O
-
Macaca fascicularis L-Ala-L-Pro + 7-amino-4-methylcoumarin
-
?

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase-4
-
Homo sapiens
dipeptidyl peptidase-4
-
Rattus norvegicus
dipeptidyl peptidase-4
-
Canis lupus familiaris
dipeptidyl peptidase-4
-
Macaca fascicularis
DPP-4
-
Homo sapiens
DPP-4
-
Rattus norvegicus
DPP-4
-
Canis lupus familiaris
DPP-4
-
Macaca fascicularis

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000069
-
-
Homo sapiens alogliptin
0.0000121
-
-
Homo sapiens sitagliptin
0.0000238
-
-
Homo sapiens vildagliptin