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Literature summary extracted from

  • Zhang, Y.; Fuessel, S.; Reimer, U.; Schutkowski, M.; Fischer, G.
    Substrate-based design of reversible Pin1 inhibitors (2002), Biochemistry, 41, 11868-11877.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.2.1.8 acetyl-Ala-Ala-D-Ser(PO3H2)-Pro-Leu-NH-4-nitroanilide IC50: 0.001 mM Homo sapiens
5.2.1.8 acetyl-Ala-Ala-D-Ser-Pro-Leu-NH-4-nitroanilide IC50: 0.085 mM Homo sapiens
5.2.1.8 Ala-Pro
-
 Homo sapiens
5.2.1.8 D-Ser(PO3H2)-Pro 1 mM, 20% inhibition Homo sapiens
5.2.1.8 Phe-Ser(PO3H2)-PSI[CS-N]-Pro-Phe-NH-4-nitroanilide IC50: 0.004 mM Homo sapiens
5.2.1.8 Phe-Ser-PSI[CS-N]-Pro-Phe-NH-4-nitroanilide IC50: 0.097 mM Homo sapiens
5.2.1.8 Ser(PO3H2)-Pro IC50: 2.0 mM Homo sapiens
5.2.1.8 Ser-Pro
-
 Homo sapiens
5.2.1.8 Ser-PSI[CS-N]-Pro
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5.2.1.8 additional information Homo sapiens enzyme is required for cell cycle progression ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
5.2.1.8 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.2.1.8 acetyl-Ala-Ala-(cis)-Pro-Ala-Lys-NH2
-
 Homo sapiens acetyl-Ala-Ala-(trans)-Pro-Ala-Lys-NH2
-
 ?
5.2.1.8 acetyl-Ala-Ala-Ser(PO3H2)-(cis)-Pro-Arg-NH-4-nitroanilide
-
 Homo sapiens acetyl-Ala-Ala-Ser(PO3H2)-(trans)-Pro-Arg-NH-4-nitroanilide
-
 ?
5.2.1.8 Ala-Ala-(cis)-Pro-Ala
-
 Homo sapiens Ala-Ala-(trans)-Pro-Ala
-
 ?
5.2.1.8 Ala-Ser(PO3H2)-(cis)-Pro
-
 Homo sapiens Ala-Ser(PO3H2)-(trans)-Pro
-
 ?
5.2.1.8 Ala-Ser(PO3H2)-(cis)-Pro-Arg
-
 Homo sapiens Ala-Ser(PO3H2)-(trans)-Pro-Arg
-
 ?
5.2.1.8 additional information no catalysis is observed with the substrates Ala-(cis)-Pro, Ala-Ala-(cis)-Pro, Ala-(cis)-Pro-Ala, Ser-(cis)-Pro and Ser(PO3H2)-(cis)-Pro Homo sapiens ?
-
 ?
5.2.1.8 additional information enzyme is required for cell cycle progression Homo sapiens ?
-
 ?
5.2.1.8 Ser(PO3H2)-(cis)-Pro-Arg
-
 Homo sapiens Ser(PO3H2)-(trans)-Pro-Arg
-
 ?
5.2.1.8 Ser(PO3H2)-(cis)-Pro-Arg-NH-4-nitroanilide
-
 Homo sapiens Ser(PO3H2)-(trans)-Pro-Arg-NH-4-nitroanilide
-
 ?
5.2.1.8 succinyl-Ala-(cis)-Pro-Phe-NH-4-nitroanilide
-
 Homo sapiens succinyl-Ala-(trans)-Pro-Phe-NH-4-nitroanilide
-
 ?
5.2.1.8 succinyl-Ala-Ala-(cis)-Pro-Phe-NH-4-nitroanilide
-
 Homo sapiens succinyl-Ala-Ala-(trans)-Pro-Phe-NH-4-nitroanilide
-
 ?

Synonyms

EC Number Synonyms Comment Organism
5.2.1.8 Pin1
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
5.2.1.8 1
-
 Ser(PO3H2)-Pro
-
 Homo sapiens
5.2.1.8 19
-
 Ala-Pro
-
 Homo sapiens
5.2.1.8 27
-
 Ser-Pro
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.2.1.8 0.001
-
 IC50: 0.001 mM Homo sapiens acetyl-Ala-Ala-D-Ser(PO3H2)-Pro-Leu-NH-4-nitroanilide
5.2.1.8 0.004
-
 IC50: 0.004 mM Homo sapiens Phe-Ser(PO3H2)-PSI[CS-N]-Pro-Phe-NH-4-nitroanilide
5.2.1.8 0.085
-
 IC50: 0.085 mM Homo sapiens acetyl-Ala-Ala-D-Ser-Pro-Leu-NH-4-nitroanilide
5.2.1.8 0.097
-
 IC50: 0.097 mM Homo sapiens Phe-Ser-PSI[CS-N]-Pro-Phe-NH-4-nitroanilide
5.2.1.8 2
-
 IC50: 2.0 mM Homo sapiens Ser(PO3H2)-Pro