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Ligands
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JZS N-[(1r)-2-amino-1-methyl-2-oxoethyl]-3-(6-methyl-4-{[3,3,3-trifluoro-2-hydroxy-2-(trifluoromethyl)propyl]amino}-1h-indazol-1-yl)benzamide
JZR Hexyl beta-D-glucopyranoside
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Code : 3K22   PDBj   RCSB PDB   PDBe
Header : TRANSCRIPTION
Title : Glucocorticoid Receptor with Bound alaninamide 10 with TIF2 peptide
Release Data : 2010-08-11
Compound :
mol_id molecule chains synonym
1 Glucocorticoid receptor A,B GR, Nuclear receptor subfamily 3 group C member 1
mutation: F602Y, C638G
mol_id molecule chains
2 Transcriptional Intermediary Factor 2 H,D
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:562)
gene: GRL, NR3C1, PGR
expression_system_strain: BL21(DE3)
expression_system_vector_type: plasmid
expression_system_plasmid: pHis GST
mol_id organism_scientific
2
synthetic: yes
other_details: Purchased
Authors : Biggadike, K.B., McLay, I.M., Madauss, K.P., Williams, S.P., Bledsoe, R.K.
Keywords : Glucocorticoid Receptor, Steroid Hormone Receptor, Nuclear Receptor, GR, glucocorticoids, alpha helical sandwich, meta-channel, Alternative initiation, Chromatin regulator, Disease mutation, DNA-binding, Isopeptide bond, Lipid-binding, Metal-binding, Nucleus, Phosphoprotein, Pseudohermaphroditism, Receptor, Steroid-binding, Transcription, Transcription regulation, Zinc-finger
Exp. method : X-RAY DIFFRACTION ( 2.100 Å )
Citation :

Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor.

Biggadike, K.,Bledsoe, R.K.,Coe, D.M.  et al.
(2009)  Proc.Natl.Acad.Sci.USA  106 : 18114 - 18119

PubMed: 19822747
DOI: 10.1073/pnas.0909125106

Chain : A, B
UniProt : P04150 (GCR_HUMAN)
Reaction : -