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International journal of molecular sciences
Dec 05, 2017;18 (12):

The FKBP51 Glucocorticoid Receptor Co-Chaperone: Regulation, Function, and Implications in Health and Disease.

Gabriel R Fries, Nils C Gassen, Theo Rein
Author Information
  1. Gabriel R Fries: Translational Psychiatry Program, Department of Psychiatry and Behavioral Sciences, McGovern Medical School, The University of Texas Health Science Center at Houston, Houston, TX 77054, USA. Gabriel.R.Fries@uth.tmc.edu.
  2. Nils C Gassen: Department of Translational Science in Psychiatry, Max Planck Institute of Psychiatry, 80804 Munich, Germany. ncgassen@psych.mpg.de.
  3. Theo Rein: Department of Translational Science in Psychiatry, Max Planck Institute of Psychiatry, 80804 Munich, Germany. theorein@psych.mpg.de. ORCID
PMID: 29206196 DOI: 10.3390/ijms18122614

Abstract

Among the chaperones and co-chaperones regulating the glucocorticoid receptor (GR), FK506 binding protein (FKBP) 51 is the most intensely investigated across different disciplines. This review provides an update on the role of the different co-chaperones of Hsp70 and Hsp90 in the regulation of GR function. The development leading to the focus on FKBP51 is outlined. Further, a survey of the vast literature on the mechanism and function of FKBP51 is provided. This includes its structure and biochemical function, its regulation on different levels-transcription, post-transcription, and post-translation-and its function in signaling pathways. The evidence portraying FKBP51 as a scaffolding protein organizing protein complexes rather than a chaperone contributing to the folding of individual proteins is collated. Finally, FKBP51's involvement in physiology and disease is outlined, and the promising efforts in developing drugs targeting FKBP51 are discussed.

Keywords

FKBP5 FKBP51 chaperone drug glucocorticoid receptor signaling pathway

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MeSH Term

Animals
Humans
Receptors, Glucocorticoid
Tacrolimus Binding Proteins

Chemicals

Receptors, Glucocorticoid
Tacrolimus Binding Proteins
tacrolimus binding protein 5
Journal Article Review
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Word Cloud

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