FKBP5 | |||||||||||||||||||||||||||||||||||||||||||||||||||
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Aliases | FKBP5, AIG6, FKBP51, FKBP54, P54, PPIase, Ptg-10, FK506 binding protein 5, FKBP prolyl isomerase 5 | ||||||||||||||||||||||||||||||||||||||||||||||||||
External IDs | OMIM: 602623; MGI: 104670; HomoloGene: 3038; GeneCards: FKBP5; OMA:FKBP5 - orthologs | ||||||||||||||||||||||||||||||||||||||||||||||||||
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Wikidata | |||||||||||||||||||||||||||||||||||||||||||||||||||
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FK506 binding protein 5, also known as FKBP5, is a protein which in humans is encoded by the FKBP5 gene.[5]
The protein encoded by this gene is a member of the immunophilin protein family, which play a role in immunoregulation and basic cellular processes involving protein folding and trafficking. This encoded protein is a cis-trans prolyl isomerase that binds to the immunosuppressants tacrolimus (FK506) and sirolimus (rapamycin). It is thought to mediate calcineurin inhibition. It also interacts functionally with mature corticoid receptor hetero-complexes (i.e. progesterone-, glucocorticoid-, mineralocorticoid-receptor complexes) along with the 90 kDa heat shock protein and PTGES3 (P23 protein).[6]
As an Hsp90-associated co-chaperone that regulates the responsiveness of steroid hormone receptors, FKBP51 plays an important role in stress endocrinology and glucocorticoid signaling.[6]
The FKBP5 gene has been found to have multiple polyadenylation sites[5] and is statistically associated with a higher rate of depressive disorders.[7]
Decreased methylation in the promoter of the FKBP5 gene has been observed in blood samples from patients with neurodegenerative diseases.[8]
As a key player in several diseases like stress-related disorders, chronic pain, and obesity, FKBP51 is an attractive drug target. SAFit2 currently the most best characterized FKBP51 ligand, has shown promising effects in numerous animal models.[6] Macrocyclic FKBP51-selective ligands are non-immunosuppressive, engage FKBP51 in cells, and block the cellular effect of FKBP51.[9]
FKBP5 has been shown to interact with Heat shock protein 90kDa alpha (cytosolic), member A1.[10]
PDB gallery
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1kt0: Structure of the Large FKBP-like Protein, FKBP51, Involved in Steroid Receptor Complexes
1kt1: Structure of the Large FKBP-like Protein, FKBP51, Involved in Steroid Receptor Complexes
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