Brand  (β version)

PDB ID: 3K23

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Ligands
Code Name Style Show Link
JZN 1-{[3-(4-{[(2r)-4-(5-fluoro-2-methoxyphenyl)-2-hydroxy-4-methyl-2-(trifluoromethyl)pentyl]amino}-6-methyl-1h-indazol-1-yl)phenyl]carbonyl}-D-prolinamide PoSSuM
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Structure summary

Code : 3K23   PDBj   RCSB PDB   PDBe
Header : TRANSCRIPTION
Title : Glucocorticoid Receptor with Bound D-prolinamide 11
Release Data : 2009-10-27
Compound :
mol_id molecule chains synonym
1 Glucocorticoid receptor A,B,C GR, Nuclear receptor subfamily 3 group C member 1
fragment: UNP residues 521-777, Ligand Binding Domain
mutation: F602Y, C638G
mol_id molecule chains synonym
2 Nuclear receptor coactivator 2 D,E,F NCoA-2, Transcriptional intermediary factor 2, hTIF2
fragment: UNP residues 740-751
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:562)
gene: GRL, NR3C1
expression_system_strain: BL21(DE3)
expression_system_vector_type: plasmid
expression_system_plasmid: pHis GST
mol_id organism_scientific
2
synthetic: yes
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, Metal-binding, Nucleus, Pseudohermaphroditism, Receptor, Steroid-binding, Transcription, Transcription regulation, Zinc-finger, Activator
Exp. method : X-RAY DIFFRACTION ( 3.000 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

Reaction

Chain : A, B, C
UniProt : P04150 (GCR_HUMAN)
Reaction : -
Chain : D, E, F
UniProt : Q15596 (NCOA2_HUMAN)
Reaction : -