• Source: FKBP5

FK506 binding protein 5, also known as FKBP5, is a protein which in humans is encoded by the FKBP5 gene.




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).
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.




Clinical significance


The FKBP5 gene has been found to have multiple polyadenylation sites and is statistically associated with a higher rate of depressive disorders.
Decreased methylation in the promoter of the FKBP5 gene has been observed in blood samples from patients with neurodegenerative diseases.




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. Macrocyclic FKBP51-selective ligands are non-immunosuppressive, engage FKBP51 in cells, and block the cellular effect of FKBP51.




Interactions


FKBP5 has been shown to interact with Heat shock protein 90kDa alpha (cytosolic), member A1.




See also


FKBP4 - a functional antagonist to FKBP5 at corticoid receptors
FKBP3 - a DNA binding FKBP




References






Further reading

Kata Kunci Pencarian:

• Daftar gen penyandi protein pada manusia/2
• FKBP5
• Genetics of post-traumatic stress disorder
• Epigenetics of anxiety and stress–related disorders
• Beck's cognitive triad
• Depression (mood)
• Elisabeth Binder
• List of human protein-coding genes 2
• Neurodegenerative disease
• List of enzymes
• Transgenerational trauma