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Literature summary extracted from
- 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.
Cloned(Commentary)
| EC Number | Cloned (Comment) | Organism |
|---|---|---|
| 3.4.14.5 | expressed using baculovirus | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.4.14.5 | 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 |  |
| 3.4.14.5 | 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 | |
| 3.4.14.5 | 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 | |
| 3.4.14.5 | 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 | |
| 3.4.14.5 | 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 | |
| 3.4.14.5 | 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 | |
| 3.4.14.5 | 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 | |
| 3.4.14.5 | 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 | |
| 3.4.14.5 | vildagliptin | i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine | Canis lupus familiaris | |
| 3.4.14.5 | vildagliptin | i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine | Homo sapiens | |
| 3.4.14.5 | vildagliptin | i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine | Macaca fascicularis | |
| 3.4.14.5 | vildagliptin | i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine | Rattus norvegicus | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.4.14.5 | Canis lupus familiaris | - |
- |
- |
| 3.4.14.5 | Homo sapiens | - |
- |
- |
| 3.4.14.5 | Macaca fascicularis | - |
- |
- |
| 3.4.14.5 | Rattus norvegicus | - |
- |
- |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 3.4.14.5 | blood plasma | - |
Homo sapiens | - |
| 3.4.14.5 | blood plasma | - |
Rattus norvegicus | - |
| 3.4.14.5 | blood plasma | - |
Canis lupus familiaris | - |
| 3.4.14.5 | blood plasma | - |
Macaca fascicularis | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.4.14.5 | L-Ala-L-Pro-7-amido-4-methylcoumarin + H2O | - |
Homo sapiens | L-Ala-L-Pro + 7-amino-4-methylcoumarin | - |
? | |
| 3.4.14.5 | L-Ala-L-Pro-7-amido-4-methylcoumarin + H2O | - |
Rattus norvegicus | L-Ala-L-Pro + 7-amino-4-methylcoumarin | - |
? | |
| 3.4.14.5 | L-Ala-L-Pro-7-amido-4-methylcoumarin + H2O | - |
Canis lupus familiaris | L-Ala-L-Pro + 7-amino-4-methylcoumarin | - |
? | |
| 3.4.14.5 | L-Ala-L-Pro-7-amido-4-methylcoumarin + H2O | - |
Macaca fascicularis | L-Ala-L-Pro + 7-amino-4-methylcoumarin | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 3.4.14.5 | dipeptidyl peptidase-4 | - |
Homo sapiens |
| 3.4.14.5 | dipeptidyl peptidase-4 | - |
Rattus norvegicus |
| 3.4.14.5 | dipeptidyl peptidase-4 | - |
Canis lupus familiaris |
| 3.4.14.5 | dipeptidyl peptidase-4 | - |
Macaca fascicularis |
| 3.4.14.5 | DPP-4 | - |
Homo sapiens |
| 3.4.14.5 | DPP-4 | - |
Rattus norvegicus |
| 3.4.14.5 | DPP-4 | - |
Canis lupus familiaris |
| 3.4.14.5 | DPP-4 | - |
Macaca fascicularis |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 3.4.14.5 | 0.0000069 | - |
- |
Homo sapiens | alogliptin | |
| 3.4.14.5 | 0.0000121 | - |
- |
Homo sapiens | sitagliptin | |
| 3.4.14.5 | 0.0000238 | - |
- |
Homo sapiens | vildagliptin | |
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