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Literature summary for 5.2.1.8 extracted from

  • Ikura, T.; Ito, N.
    Peptidyl-prolyl isomerase activity of FK506 binding protein 12 prevents tau peptide from aggregating (2013), Protein Eng. Des. Sel., 26, 539-546.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression of wild-type and mutant enzymes Homo sapiens

Protein Variants

Protein Variants Comment Organism
V55R site-directed mutagenesis, the mutation increases the PPIase activity by a factor of 11 Homo sapiens
Y82K site-directed mutagenesis, the mutation decreases the PPIase activity by a factor of 7 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
FK506
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
FK506 binding protein 12
-
Homo sapiens
FKBP 12
-
Homo sapiens
peptidyl-prolyl isomerase
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
assay at Homo sapiens

General Information

General Information Comment Organism
physiological function peptidyl-prolyl isomerase activity of FKBP12 is essential for prevention of aggregation of tau, an Alzheimer's disease-related protein. Tau aggregates into neurofibrillary tangles when it is hyperphosphorylated, only the cis-isomer can aggregate. FKBP12 catalyzes isomerization of the tau R3 peptide peptide in both the monomeric and aggregative states, once the cis-isomer is converted into the trans-isomer in the aggregative state, the trans-isomer is quickly released from the aggregation because the trans-isomer cannot aggregate, inhibitory mechanism of R3 peptide aggregation by simple binding of FKBP12, overview. IC50 of FKBP12 is 0.003 mM. The aggregation inhibitory activity of FKBP12 is independent of the affinity between FKBP12 and the R3 peptide. Therefore, the aggregation inhibitory activity of FKBP12 depends only on the PPIase activity of FKBP12 Homo sapiens