AR Protein Crystal

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.

Protein Classification

Ligand Binding Protein

Structure Weight

29541.62 Da

Polymer

1

Molecule

Androgen receptor

Chain Length

250 amino acids

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 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

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