scholarly journals Drug Design Approaches to Manipulate the Agonist-Antagonist Equilibrium in Steroid Receptors

10.5772/28124 ◽  
2012 ◽  
Author(s):  
Scott J. ◽  
Paolo Conti ◽  
Wim Dokter ◽  
Pedro H. ◽  
Jacob de
Keyword(s):  
Drug Design ◽  
Steroid Receptors

Role of molecular chaperones in steroid receptor action

2004 ◽  
Vol 40 ◽  
pp. 41-58 ◽  
Author(s):  
William B Pratt ◽  
Mario D Galigniana ◽  
Yoshihiro Morishima ◽  
Patrick J M Murphy
Keyword(s):  
Transcriptional Activation ◽  
Protein Trafficking ◽  
Steroid Receptors ◽  
Transcriptional Regulatory ◽  
Ubiquitin Proteasome ◽  
Proteasome Pathway ◽  
Receptor Action ◽  
Binding Cleft ◽  
Hsp 90

Unliganded steroid receptors are assembled into heterocomplexes with heat-shock protein (hsp) 90 by a multiprotein chaperone machinery. In addition to binding the receptors at the chaperone site, hsp90 binds cofactors at other sites that are part of the assembly machinery, as well as immunophilins that connect the assembled receptor-hsp90 heterocomplexes to a protein trafficking pathway. The hsp90-/hsp70-based chaperone machinery interacts with the unliganded glucocorticoid receptor to open the steroid-binding cleft to access by a steroid, and the machinery interacts in very dynamic fashion with the liganded, transformed receptor to facilitate its translocation along microtubular highways to the nucleus. In the nucleus, the chaperone machinery interacts with the receptor in transcriptional regulatory complexes after hormone dissociation to release the receptor and terminate transcriptional activation. By forming heterocomplexes with hsp90, the chaperone machinery stabilizes the receptor to degradation by the ubiquitin-proteasome pathway of proteolysis.

Steroid Receptors as Molecular Targets for Cancer Diagnosis and Therapy

2009 ◽  
Vol 26 (3) ◽  
pp. 207-273 ◽  
Author(s):  
Pramod Mishra ◽  
Arvind Gulbake ◽  
Aviral Jain ◽  
Piush Khare ◽  
Vandana Soni ◽  
...  
Keyword(s):  
Cancer Diagnosis ◽  
Steroid Receptors ◽  
Molecular Targets ◽  
Diagnosis And Therapy ◽  
Cancer Diagnosis And Therapy
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