In:
ChemMedChem, Wiley, Vol. 7, No. 8 ( 2012-08), p. 1351-1359
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.
Type of Medium:
Online Resource
ISSN:
1860-7179
,
1860-7187
DOI:
10.1002/cmdc.201200137
Language:
English
Publisher:
Wiley
Publication Date:
2012
detail.hit.zdb_id:
2209649-8
SSG:
15,3
Permalink