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AR Protein Crystal

(CBCRY23)  Download Datasheet
Background
Background
Androgen receptor (AR) is a ligand-inducible steroid hormone receptor that mediates androgen action, determining male sexual phenotypes and promoting spermatogenesis. As the androgens play a dominant role in male sexual development and function, steroidal androgen agonists have been used clinically for some years. However, there is a risk of potential side effects and most steroidal androgens cannot be dosed orally, which limits the use of these substances. 1,2-Dihydro-6-N,N-bis(2,2,2-trifluoroethyl)amino-4-trifluoromethyl-2-quinolinone (LGD2226) is a synthetic nonsteroidal ligand and a novel selective AR modulator.
Molecular Description
Protein Classification
Ligand Binding Protein
Structure Weight
29541.62 Da
Polymer
1
Molecule
Androgen receptor
Chain Length
250 amino acids
Crystal Description
PDB ID
2HVC
MMDB ID
53414
Source
E.coli
Method
X-Ray Diffraction
Resolution
2.8Å
Ligand Chemical Component
6-[Bis(2,2,2-Trifluoroethyl)Amino]-4-(Trifluoromethyl)quinolin-2(1H)-one.
Gene Information
Gene Name
AR
Synonyms
RP11-383C12.1; AIS, DHTR; HUMARA; HYSP1; KD; NR3C4; SBMA; SMAX1; TFM; OTTHUMP00000023450; OTTHUMP00000061928; dihydrotestosterone receptor; Nuclear receptor subfamily 3 group C member 4; spinal and bulbar muscular atrophy
UniProt ID
P10275
Gene ID
367
Chromosome Location
Xq11.2-q12
Function
androgen binding; androgen receptor activity; metal ion binding; receptor activity; protein dimerization activity; receptor binding; sequence-specific DNA binding; transcription factor activity; zinc ion binding
Reference
Reference
Wang, F., Liu, X.-Q., Li, H., Liang, K.-N., Miner, J.N., Hong, M., Kallel, E.A., van Oeveren, A., Zhi, L., Jiang, T. (2006) Structure of the ligand-binding domain (LBD) of human androgen receptor in complex with a selective modulator LGD2226 ACTA CRYSTALLOGR.,SECT.F 62: 1067-1071