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Publication : A new first step in activation of steroid receptors: hormone-induced switching of FKBP51 and FKBP52 immunophilins.

First Author  Davies TH Year  2002
Journal  J Biol Chem Volume  277
Issue  7 Pages  4597-600
PubMed ID  11751894 Mgi Jnum  J:74637
Mgi Id  MGI:2158896 Doi  10.1074/jbc.C100531200
Citation  Davies TH, et al. (2002) A new first step in activation of steroid receptors: hormone-induced switching of FKBP51 and FKBP52 immunophilins. J Biol Chem 277(7):4597-600
abstractText  We have identified a new first step in the hormonal activation of the glucocorticoid receptor (GR). Rather than causing immediate dissociation of the cytoplasmic GR heterocomplex, binding of hormone-induced substitution of one immunophilin (FKBP51) for another (FKBP52), and concomitant recruitment of the transport protein dynein while leaving Hsp90 unchanged. Immunofluorescence and fractionation revealed hormone-induced translocation of the hormone-generated GR-Hsp90-FKBP52-dynein complex from cytoplasm to nucleus, a step that precedes dissociation of the complex within the nucleus and conversion of GR to the DNA-binding form. Taken as a whole, these studies identify immunophilin interchange as the earliest known event in steroid receptor signaling and provide the first evidence of differential roles for FKBP51 and FKBP52 immunophilins in the control of steroid receptor subcellular localization and transport.
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