Target intelligence / Profile preview

Peptidyl-prolyl cis-trans isomerase FKBP1A (FKBP1A)

Target
FKBP1A
Molecular classification
Enzyme, Peptidyl-prolyl cis-trans isomerase, Immunophilin
01

Overview

Peptidyl-prolyl cis-trans isomerase FKBP1A, also known as FKBP12, is a member of the immunophilin protein family. It functions primarily as a peptidyl-prolyl cis-trans isomerase (PPIase), catalyzing the interconversion between cis and trans forms of proline imidic peptide bonds in oligopeptides, thereby accelerating protein folding. It binds immunosuppressive drugs such as tacrolimus (FK506) and sirolimus (rapamycin), and regulates intracellular signaling.

Other names
FKBP12Calstabin-1RotamaseImmunophilin FKBP12
02

Mechanism of action

Inhibition of calcineurin or mTOR pathways through formation of drug-protein complexes

03

Biological functions

Protein folding/maturationRegulation of TGF-beta/activin signalingCalcium channel modulationCis-trans isomerization of proline residues
04

Disease associations

Congenital heart disordersNoncompaction of left ventricular myocardium
05

Safety considerations

ImmunosuppressionPotential for congenital heart disorders (based on mouse homolog studies)
06

Interacting drugs

Tacrolimus (FK506)

1 more in the full profile.

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