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Literature summary for 3.4.14.5 extracted from

  • Connolly, B.A.; Sanford, D.G.; Chiluwal, A.K.; Healey, S.E.; Peters, D.E.; Dimare, M.T.; Wu, W.; Liu, Y.; Maw, H.; Zhou, Y.; Li, Y.; Jin, Z.; Sudmeier, J.L.; Lai, J.H.; Bachovchin, W.W.
    Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety (2008), J. Med. Chem., 51, 6005-6013.
    View publication on PubMed

Application

Application Comment Organism
medicine DPP-IV is a target for the treatment of type 2 diabetes Mus musculus
medicine DPP-IV is a target for the treatment of type 2 diabetes Homo sapiens
medicine DPP-IV is a target for the treatment of type 2 diabetes Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
H-(S)-alaninyl-(R)-boro-proline
-
Homo sapiens
H-(S)-alaninyl-(R)-boro-proline
-
Mus musculus
H-(S)-alaninyl-(R)-boro-proline
-
Rattus norvegicus
H-(S)-Glu-(R)-boro-alanine
-
Homo sapiens
H-(S)-Glu-(R)-boro-alanine
-
Mus musculus
H-(S)-Glu-(R)-boro-alanine
-
Rattus norvegicus
H-(S)-glutaminyl-(R)-boro-alanine
-
Homo sapiens
H-(S)-glutaminyl-(R)-boro-alanine
-
Mus musculus
H-(S)-glutaminyl-(R)-boro-alanine
-
Rattus norvegicus
H-(S)-glutamyl-(R)-boro-proline
-
Homo sapiens
H-(S)-glutamyl-(R)-boro-proline
-
Mus musculus
H-(S)-glutamyl-(R)-boro-proline
-
Rattus norvegicus
H-(S)-valinyl-(R)-boro-alanine
-
Homo sapiens
H-(S)-valinyl-(R)-boro-alanine
-
Mus musculus
H-(S)-valinyl-(R)-boro-alanine
-
Rattus norvegicus
H-(S)-valinyl-(R)-boro-proline
-
Homo sapiens
H-(S)-valinyl-(R)-boro-proline
-
Mus musculus
H-(S)-valinyl-(R)-boro-proline
-
Rattus norvegicus
H-glycyl-(R)-boro-proline
-
Homo sapiens
H-glycyl-(R)-boro-proline
-
Mus musculus
H-glycyl-(R)-boro-proline
-
Rattus norvegicus
N-acetyl-(S)-valinyl-(R)-boro-proline
-
Homo sapiens
N-acetyl-(S)-valinyl-(R)-boro-proline
-
Mus musculus
N-acetyl-(S)-valinyl-(R)-boro-proline
-
Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
glucagon-like peptide 1 + H2O Mus musculus
-
?
-
?
glucagon-like peptide 1 + H2O Homo sapiens
-
?
-
?
glucagon-like peptide 1 + H2O Rattus norvegicus
-
?
-
?
glucose-dependent insulinotropic peptide + H2O Mus musculus
-
?
-
?
glucose-dependent insulinotropic peptide + H2O Homo sapiens
-
?
-
?
glucose-dependent insulinotropic peptide + H2O Rattus norvegicus
-
?
-
?

Organism

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

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Mus musculus
-
blood plasma
-
Rattus norvegicus
-
placenta
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glucagon-like peptide 1 + H2O
-
Mus musculus ?
-
?
glucagon-like peptide 1 + H2O
-
Homo sapiens ?
-
?
glucagon-like peptide 1 + H2O
-
Rattus norvegicus ?
-
?
glucose-dependent insulinotropic peptide + H2O
-
Mus musculus ?
-
?
glucose-dependent insulinotropic peptide + H2O
-
Homo sapiens ?
-
?
glucose-dependent insulinotropic peptide + H2O
-
Rattus norvegicus ?
-
?
L-Ala-L-Pro-4-nitroanilide
-
Mus musculus L-Ala-L-Pro + 4-nitroaniline
-
?
L-Ala-L-Pro-4-nitroanilide
-
Homo sapiens L-Ala-L-Pro + 4-nitroaniline
-
?
L-Ala-L-Pro-4-nitroanilide
-
Rattus norvegicus L-Ala-L-Pro + 4-nitroaniline
-
?

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase IV
-
Mus musculus
dipeptidyl peptidase IV
-
Homo sapiens
dipeptidyl peptidase IV
-
Rattus norvegicus
DPP-IV
-
Mus musculus
DPP-IV
-
Homo sapiens
DPP-IV
-
Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000000018
-
H-(S)-valinyl-(R)-boro-proline in 0.1 M HEPES, 0.14 M NaCl, pH 8.0, at 25°C Homo sapiens
0.000000027
-
H-(S)-alaninyl-(R)-boro-proline in 0.1 M HEPES, 0.14 M NaCl, pH 8.0, at 25°C Homo sapiens
0.0000004
-
H-glycyl-(R)-boro-proline in 0.1 M HEPES, 0.14 M NaCl, pH 8.0, at 25°C Homo sapiens
0.0000018
-
H-(S)-glutamyl-(R)-boro-proline in 0.1 M HEPES, 0.14 M NaCl, pH 8.0, at 25°C Homo sapiens
0.0000039
-
H-(S)-valinyl-(R)-boro-alanine in 0.1 M HEPES, 0.14 M NaCl, pH 8.0, at 25°C Homo sapiens
0.0000083
-
H-(S)-Glu-(R)-boro-alanine in 0.1 M HEPES, 0.14 M NaCl, pH 8.0, at 25°C Homo sapiens
0.000017
-
H-(S)-glutaminyl-(R)-boro-alanine in 0.1 M HEPES, 0.14 M NaCl, pH 8.0, at 25°C Homo sapiens
0.0033
-
N-acetyl-(S)-valinyl-(R)-boro-proline in 0.1 M HEPES, 0.14 M NaCl, pH 8.0, at 25°C Homo sapiens