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The prospect of FKBP51 as a drug target.
ChemMedChem. 2012 Aug; 7(8):1351-9.C

Abstract

The FK506 binding protein 51 (FKBP51) is best known as an Hsp90-associated co-chaperone that regulates the responsiveness of steroid hormone receptors. In human genetic association studies, FKBP51 has repeatedly been associated with emotion processing and numerous stress-related affective disorders. It has also been implicated in contributing to the glucocorticoid hyposensitivity observed in New World primates. More recently, several research groups have consistently shown a protective effect of FKBP51 knockout or knockdown on stress endocrinology and stress-coping behavior in animal models of depression and anxiety. The principal druggability of FKBP51 is exemplified by the prototypic FKBP ligands FK506 and rapamycin. Moreover, FKBP51 is highly suited for X-ray co-crystallography, which should facilitate the rational drug design of improved FKBP51 ligands. In summary, FKBP51 has emerged as a promising new drug target for stress-related disorders that should be amenable to drug discovery.

Links

Publisher Full Text (DOI)

Authors+Show Affiliations

Schmidt MV
Max Planck Institute of Psychiatry, Kraepelinstrasse 2-10, 80804 Munich (Germany).
Paez-Pereda M
No affiliation info available
Holsboer F
No affiliation info available
Hausch F
No affiliation info available

MeSH

AnimalsAntidepressive AgentsDepressive DisorderDrug DesignEnergy MetabolismGene Knockdown TechniquesHSP90 Heat-Shock ProteinsHumansLigandsMiceMice, KnockoutPolymorphism, Single NucleotideReceptors, SteroidTacrolimus Binding Proteins

Pub Type(s)

Journal Article

Language

eng

PubMed ID

22581765

Citation

Schmidt, Mathias V., et al. "The Prospect of FKBP51 as a Drug Target." ChemMedChem, vol. 7, no. 8, 2012, pp. 1351-9.
Schmidt MV, Paez-Pereda M, Holsboer F, et al. The prospect of FKBP51 as a drug target. ChemMedChem. 2012;7(8):1351-9.
Schmidt, M. V., Paez-Pereda, M., Holsboer, F., & Hausch, F. (2012). The prospect of FKBP51 as a drug target. ChemMedChem, 7(8), 1351-9. https://doi.org/10.1002/cmdc.201200137
Schmidt MV, et al. The Prospect of FKBP51 as a Drug Target. ChemMedChem. 2012;7(8):1351-9. PubMed PMID: 22581765.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The prospect of FKBP51 as a drug target. AU - Schmidt,Mathias V, AU - Paez-Pereda,Marcelo, AU - Holsboer,Florian, AU - Hausch,Felix, Y1 - 2012/05/13/ PY - 2012/03/13/received PY - 2012/04/13/revised PY - 2012/5/15/entrez PY - 2012/5/15/pubmed PY - 2012/12/10/medline SP - 1351 EP - 9 JF - ChemMedChem JO - ChemMedChem VL - 7 IS - 8 N2 - The FK506 binding protein 51 (FKBP51) is best known as an Hsp90-associated co-chaperone that regulates the responsiveness of steroid hormone receptors. In human genetic association studies, FKBP51 has repeatedly been associated with emotion processing and numerous stress-related affective disorders. It has also been implicated in contributing to the glucocorticoid hyposensitivity observed in New World primates. More recently, several research groups have consistently shown a protective effect of FKBP51 knockout or knockdown on stress endocrinology and stress-coping behavior in animal models of depression and anxiety. The principal druggability of FKBP51 is exemplified by the prototypic FKBP ligands FK506 and rapamycin. Moreover, FKBP51 is highly suited for X-ray co-crystallography, which should facilitate the rational drug design of improved FKBP51 ligands. In summary, FKBP51 has emerged as a promising new drug target for stress-related disorders that should be amenable to drug discovery. SN - 1860-7187 UR - https://www.unboundmedicine.com/medline/citation/22581765/The_prospect_of_FKBP51_as_a_drug_target_ L2 - https://doi.org/10.1002/cmdc.201200137 DB - PRIME DP - Unbound Medicine ER -