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Literature summary for 5.2.1.8 extracted from

  • Duncan, K.E.; Dempsey, B.R.; Killip, L.E.; Adams, J.; Bailey, M.L.; Lajoie, G.A.; Litchfield, D.W.; Brandl, C.J.; Shaw, G.S.; Shilton, B.H.
    Discovery and characterization of a nonphosphorylated cyclic peptide inhibitor of the peptidylprolyl isomerase, Pin1 (2011), J. Med. Chem., 54, 3854-3865.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
cyclic CRYPEVEIC the cyclic peptide is specific for the active site of the PPIase domain Homo sapiens
linear CRYPEVEIC
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
glutathione-Sepharose column chromatography and S-Sepharose column chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
succinyl-Ala-Glu-(cis)-Pro-Phe-4-nitroanilide
-
Homo sapiens succinyl-Ala-Glu-(trans)-Pro-Phe-4-nitroanilide
-
?
Trp-Phe-Tyr-pSer-Pro-Arg-4-nitroanilide
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
peptidylprolyl isomerase
-
Homo sapiens
Pin1
-
Homo sapiens
PPIase
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0002
-
cyclic CRYPEVEIC using Trp-Phe-Tyr-pSer-Pro-Arg-4-nitroanilide as substrate, in 50 mM HEPES, 0.1 M NaCl, 5 mM NaN3, pH 7.4, at 22°C Homo sapiens
0.00052
-
cyclic CRYPEVEIC using succinyl-Ala-Glu-(cis)-Pro-Phe-4-nitroanilide as substrate, in 50 mM HEPES, 0.1 M NaCl, 5 mM NaN3, pH 7.4, at 22°C Homo sapiens
0.044
-
linear CRYPEVEIC using succinyl-Ala-Glu-(cis)-Pro-Phe-4-nitroanilide as substrate, in 50 mM HEPES, 0.1 M NaCl, 5 mM NaN3, pH 7.4, at 22°C Homo sapiens