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ChemMedChem. 2012 Aug;7(8):1351-9. doi: 10.1002/cmdc.201200137. Epub 2012 May 13.

The prospect of FKBP51 as a drug target.

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  • 1Max Planck Institute of Psychiatry, Kraepelinstrasse 2-10, 80804 Munich (Germany).


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.

Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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