Английская Википедия:FKBP5
Шаблон:Short description Шаблон:Infobox gene FK506 binding protein 5, also known as FKBP5, is a protein which in humans is encoded by the FKBP5 gene.[1]
Function
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).[2]
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.[2]
Clinical significance
The FKBP5 gene has been found to have multiple polyadenylation sites[1] and is statistically associated with a higher rate of depressive disorders.[3]
Decreased methylation in the promoter of the FKBP5 gene has been observed in blood samples from patients with neurodegenerative diseases.[4]
FKBP51 Ligands
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.[2] Macrocyclic FKBP51-selective ligands are non-immunosuppressive, engage FKBP51 in cells, and block the cellular effect of FKBP51.[5]
Interactions
FKBP5 has been shown to interact with Heat shock protein 90kDa alpha (cytosolic), member A1.[6]
See also
References
Further reading
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