Linked Life Data

8910505

Source:http://linkedlifedata.com/resource/pubmed/id/8910505

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
45
pubmed:dateCreated
1996-12-30
pubmed:abstractText
The regulation of human androgen receptor (AR) by the molecular chaperone Hsp90 was investigated using the yeast Saccharomyces cerevisiae as a model system. These studies were performed in strains expressing a conditional temperature-sensitive mutant allele of the hsp82 gene, which encodes Hsp90 protein. At the restrictive temperature in the mutant, there is a decrease in hormone-dependent transactivation by the AR, although steady state levels of AR protein are unchanged. Quantitative hormone binding studies at the permissive temperature revealed the presence of both high affinity and low affinity hormone binding states. At the restrictive temperature in the hsp82 mutant, the high affinity state was abolished, and only the low affinity state was observed. The change in hormone binding affinity was further investigated by a competition assay with the anti-androgen hydroxyflutamide. Under permissive conditions, hydroxyflutamide competes poorly for the synthetic androgen R1881, but under restrictive conditions in the hsp82 mutant strain, hydroxyflutamide was shown to be a potent competitive inhibitor. Our findings indicate that Hsp90 participates in the activation process by maintaining apoAR in a high affinity ligand binding conformation which is important for efficient response to hormone.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Nov
pubmed:issn
0021-9258
pubmed:author
pubmed:issnType
Print
pubmed:day
8
pubmed:volume
271
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
28697-702
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1996
pubmed:articleTitle
Hsp90 regulates androgen receptor hormone binding affinity in vivo.
pubmed:affiliation
Department of Cell Biology and Anatomy, Mount Sinai Medical Center, New York New York 10029, USA. caplan@msvax.mssm.edu
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't