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The FKBP51-Glucocorticoid Receptor Balance in Stress-Related Mental Disorders.
Curr Mol Pharmacol. 2015; 9(2):126-40.CM

Abstract

The immunophilin FK506 binding protein 51 (FKBP51) has emerged as one of the most intensely investigated proteins in stress-related mental disorders. It was originally characterized as Hsp90 cochaperone and part of the receptor-chaperone heterocomplex that governs the activity of steroid receptors. It turned out that the presence of FKBP51 in this heterocomplex leads to diminished activity of the corticosteroid receptors. In particular, based on its inhibitory action on the glucocorticoid receptor (GR), FKBP51 was included in a candidate gene approach to discover gene polymorphisms that might be relevant for the development and treatment of major depression. The discovery that polymorphisms in the gene coding for FKBP51 were linked to the treatment response of depressed patients intensified the research on the role of FKBP51 in stress-related diseases worldwide. It has become evident that FKBP51 is not only a regulator of GR action, but also a GR target. The function of this ultrashort intracellular feedback loop is critically important for cellular and physiological stress regulation as it does not only calibrate the function of GR, but also the levels of FKBP51. Given the pleiotropic functions of FKBP51, its levels might be equally important for mental disorders as GR function and hence for the development of potential FKBP51 drug targets.

Authors+Show Affiliations

No affiliation info availableNo affiliation info availableNo affiliation info availableDepartment of Translational Research in Psychiatry, Max Planck Institute of Psychiatry, Munich, Germany. theorein@mpipsykl.mpg.de.

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

25986564

Citation

Fries, Gabriel R., et al. "The FKBP51-Glucocorticoid Receptor Balance in Stress-Related Mental Disorders." Current Molecular Pharmacology, vol. 9, no. 2, 2015, pp. 126-40.
Fries GR, Gassen NC, Schmidt U, et al. The FKBP51-Glucocorticoid Receptor Balance in Stress-Related Mental Disorders. Curr Mol Pharmacol. 2015;9(2):126-40.
Fries, G. R., Gassen, N. C., Schmidt, U., & Rein, T. (2015). The FKBP51-Glucocorticoid Receptor Balance in Stress-Related Mental Disorders. Current Molecular Pharmacology, 9(2), 126-40.
Fries GR, et al. The FKBP51-Glucocorticoid Receptor Balance in Stress-Related Mental Disorders. Curr Mol Pharmacol. 2015;9(2):126-40. PubMed PMID: 25986564.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The FKBP51-Glucocorticoid Receptor Balance in Stress-Related Mental Disorders. AU - Fries,Gabriel R, AU - Gassen,Nils C, AU - Schmidt,Ulrike, AU - Rein,Theo, PY - 2015/04/20/received PY - 2015/05/17/accepted PY - 2015/5/20/entrez PY - 2015/5/20/pubmed PY - 2016/10/7/medline SP - 126 EP - 40 JF - Current molecular pharmacology JO - Curr Mol Pharmacol VL - 9 IS - 2 N2 - The immunophilin FK506 binding protein 51 (FKBP51) has emerged as one of the most intensely investigated proteins in stress-related mental disorders. It was originally characterized as Hsp90 cochaperone and part of the receptor-chaperone heterocomplex that governs the activity of steroid receptors. It turned out that the presence of FKBP51 in this heterocomplex leads to diminished activity of the corticosteroid receptors. In particular, based on its inhibitory action on the glucocorticoid receptor (GR), FKBP51 was included in a candidate gene approach to discover gene polymorphisms that might be relevant for the development and treatment of major depression. The discovery that polymorphisms in the gene coding for FKBP51 were linked to the treatment response of depressed patients intensified the research on the role of FKBP51 in stress-related diseases worldwide. It has become evident that FKBP51 is not only a regulator of GR action, but also a GR target. The function of this ultrashort intracellular feedback loop is critically important for cellular and physiological stress regulation as it does not only calibrate the function of GR, but also the levels of FKBP51. Given the pleiotropic functions of FKBP51, its levels might be equally important for mental disorders as GR function and hence for the development of potential FKBP51 drug targets. SN - 1874-4702 UR - https://www.unboundmedicine.com/medline/citation/25986564/The_FKBP51_Glucocorticoid_Receptor_Balance_in_Stress_Related_Mental_Disorders_ DB - PRIME DP - Unbound Medicine ER -