AR, Androgen Receptor

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AR Protein Crystal(CBCRY23)

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Product Summary
Name	AR Protein Crystal 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.

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

AR Protein Crystal

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AR Protein Crystal(CBCRY23)

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