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Literature summary for 3.4.14.5 extracted from

  • Jost, M.M.; Lamerz, J.; Tammen, H.; Menzel, C.; De Meester, I.; Lambeir, A.M.; Augustyns, K.; Scharpe, S.; Zucht, H.D.; Rose, H.; Juergens, M.; Schulz-Knappe, P.; Budde, P.
    In vivo profiling of DPP4 inhibitors reveals alterations in collagen metabolism and accumulation of an amyloid peptide in rat plasma (2009), Biochem. Pharmacol., 77, 228-237.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine vildagliptin, reversible inhibitor Homo sapiens
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine vildagliptin, reversible inhibitor, vildagliptin inhibits DPP4 activity by about 50% at a dosage of 0.3 mg/kg body weight Rattus norvegicus
bis(4-acetamidophenyl) 1-(S)-prolylpyrrolidine-2(R,S)-phosphonate AB-192, irreversible inhibitor Homo sapiens
bis(4-acetamidophenyl) 1-(S)-prolylpyrrolidine-2(R,S)-phosphonate AB-192, irreversible inhibitor, AB-192 sufficiently inhibits DPP4 only in the higher dosage range of more than 1mg/kg body weight Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.014
-
BRI peptide (1-23) in 40 mM HEPES-buffer, pH 7.4, at 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Rattus norvegicus
-
semen
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
BRI peptide (1-23) + H2O
-
Homo sapiens ?
-
?
Gly-L-Pro-4-nitroanilide
-
Homo sapiens Gly-L-Pro + 4-nitroaniline
-
?
Gly-L-Pro-4-nitroanilide
-
Rattus norvegicus Gly-L-Pro + 4-nitroaniline
-
?

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase 4
-
Homo sapiens
dipeptidyl peptidase 4
-
Rattus norvegicus
DPP4
-
Homo sapiens
DPP4
-
Rattus norvegicus

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
5.2
-
BRI peptide (1-23) in 40 mM HEPES-buffer, pH 7.4, at 37°C Homo sapiens