http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1375517-A1

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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K14-72
filingDate 2003-06-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3936ceaafdaf01857ee5a91875acc6a3
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7267ad74174ba2ab8af6edce6837f42f
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publicationDate 2004-01-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-1375517-A1
titleOfInvention Structure of a glucocorticoid receptor ligand binding domain comprising an expanded binding pocket and methods employing same
abstract A solved three-dimensional crystal structure of a glucocorticordnreceptor (GR) α ligand binding domain polypeptide is disclosed, in the form ofna crystalline glucocorticord receptor α ligand binding domain polypeptide inncomplex with the ligand fluticasone propionate (FP) and a peptide derivednfrom the co-activator TIF2. The GR/FP/TIF2 structure includes an expandednbinding pocket not seen in other GR structures. Methods of designing steroidnand non-steroid modulators of the biological activity of GR and other nuclearnreceptors (NRs) are also disclosed. In another aspect of the present inventionnhomology models of androgen receptor (AR), progesterone receptor (PR) andnmineralcorticoid receptor (MR) are disclosed, as well as methods of formingnhomology models for other NRs. Methods of forming a soluble GR/FP/TIF2ncomplex are also disclosed.
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