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Literature summary for 5.2.1.8 extracted from

  • Uchida, T.; Takamiya, M.; Takahashi, M.; Miyashita, H.; Ikeda, H.; Terada, T.; Matsuo, Y.; Shirouzu, M.; Yokoyama, S.; Fujimori, F.; Hunter, T.
    Pin1 and Par14 peptidyl prolyl isomerase inhibitors block cell proliferation (2003), Chem. Biol., 10, 15-24.
    View publication on PubMed
Search for more literature for 5.2.1.8

Application

Application Comment Organism
medicine Pin1 inhibitors can be used as a novel type of anticancer drug that acts by blocking cell cycle progression Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
2,7-dimethylbenzo[lmn][3,8]phenanthroline-1,3,6,8(2H,7H)-tetrone IC50: 0.002 mM Mus musculus
diethyl 1,3,8,10-tetrahydro-1,3,8,10-tetraoxoanthra[2,1,9-def:6,5,10-d'e'f']diisoquinoline-2,9-diacetate IC50: 0.0015 mM Mus musculus
diethyl-1,3,6,8-tetrahydro-1,3,6,8-tetraoxobenzo[lmn][3,8]phenanthroline 2,7-diacetate IC50: 0.0015 mM, inhibitor with the least non-specific toxicity Mus musculus
additional information Pin1 inhibitors may be used as a novel type of anticancer drug that acts by blocking cell cycle progression Mus musculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.12
-
 succinyl-Ala-Glu-Pro-Phe-7-amido-4-methylcoumarin
-
 Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Mus musculus the enzyme is involved in cell cycle progression ?
-
 ?

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information the enzyme is involved in cell cycle progression Mus musculus ?
-
 ?
succinyl-Ala-Glu-(trans)-Pro-Phe-7-amido-4-methylcoumarin
-
 Mus musculus succinyl-Ala-Glu-(cis)-Pro-Phe-7-amido-4-methylcoumarin
-
 r

Synonyms

Synonyms Comment Organism
Pin1
-
 Mus musculus
PPIase
-
 Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0015
-
 IC50: 0.0015 mM Mus musculus diethyl 1,3,8,10-tetrahydro-1,3,8,10-tetraoxoanthra[2,1,9-def:6,5,10-d'e'f']diisoquinoline-2,9-diacetate
0.0015
-
 IC50: 0.0015 mM, inhibitor with the least non-specific toxicity Mus musculus diethyl-1,3,6,8-tetrahydro-1,3,6,8-tetraoxobenzo[lmn][3,8]phenanthroline 2,7-diacetate
0.002
-
 IC50: 0.002 mM Mus musculus 2,7-dimethylbenzo[lmn][3,8]phenanthroline-1,3,6,8(2H,7H)-tetrone