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FK506 Binding Protein
- Molecular classification
- Enzyme, Peptidyl-prolyl cis-trans isomerase, Immunophilin
01
Overview
FK506 binding proteins (FKBPs) are a family of highly conserved proteins found in all eukaryotes. They possess *cis/trans* peptidyl-prolyl isomerase (PPIase) activity, catalyzing the interconversion between proline residues in polypeptides, assisting in protein folding, modulating signaling pathways, and regulating apoptosis and transcription. FKBPs are best known as intracellular receptors for the immunosuppressive drugs FK506 (tacrolimus) and rapamycin (sirolimus). When bound to these drugs, FKBPs form complexes that inhibit specific phosphatases (calcineurin) or kinases (mTOR), affecting immune response, cell growth, and proliferation.
- Other names
- ImmunophilinsFKBP12FKBP25FKBP52FKBP51
02
Mechanism of action
The FK506-FKBP12 complex inhibits calcineurin, blocking T-cell activation. The rapamycin-FKBP12 complex targets mTOR kinase, affecting cell growth and proliferation pathways.
03
Biological functions
Protein foldingSignal transductionApoptosisTranscriptionImmune responseCell proliferationRegulation of calcium channelsModulation of TGF-beta receptor signaling
04
Disease associations
CancerOrgan transplant rejectionOther (cellular growth control)Cell cycle arrest
05
Safety considerations
Immunosuppression-related side effects associated with tacrolimus and rapamycin
06
Interacting drugs
Tacrolimus (FK506)
1 more in the full profile.
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