Androgen receptor

From Proteopedia

Template:STRUCTURE 2q7i

Androgen receptor (AR) is a nuclear receptor which is activated by testosterone or 5-α-dihydrotestosterone (DHT). Upon binding the androgenic hormone it translocates to the nucleus where it acts as a DNA-binding transcription factor. The AR binds to a specific sequence of DNA called hormone response element. AR binds to other proteins in the nucleus causing up- or down gene regulation. AR exists in two isoforms. AR-B is full length 110 kDa and AR-A (87 kDa) lacks the N-terminal 187 amino acids. AR is composed of 5 domains -
A/B: N-terminal contains the activation functions and dimerization surface
C: DNA binding domain (DBD)
D: Hinge region between DBD and LBD
E: Ligand binding domain (LBD) which binds the N-terminal FXXFL motif
F: C-terminal domain

3D Structures of androgen receptor

Updated on 29-April-2013

AR DBD domain

1r4i – rAR (mutant) + DNA – rat

AR LBD domain

AR LBD domain complex with testosterone or DHT

1i37 – rAR + DHT
1i38 – rAR (mutant) + DHT
2ama – hAR + DHT - human
1t7t – cAR + DHT - chimpanzee
2ylo, 2ylp, 2ylq, 3zqt, 4hlw – hAR + testosterone + benzoate derivative
2pio, 2pip, 2piq, 2pir, 2pit, 2piu, 2piv, 2piw, 2pix, 2pkl, 2qpy – hAR + DHT + small molecule
2yhd – hAR + testosterone + small molecule
2am9 – rAR + testosterone

Other AR LBD domain complexes

1e3g, 1xq3 – hAR + androgen
1gs4 – hAR (mutant) + corticosteroid
1z95, 3rlj – hAR + anti-androgen
2oz7, 3rll – hAR (mutant) + anti-androgen
2ax6, 2ax7, 2ax8 – hAR (mutant) + nonsteroidal ligand
2ax9, 2axa – hAR + nonsteroidal ligand
2amb, 2pnu – hAR + steroid
1xnn – rAR (mutant) + nonsteroidal ligand
2ihq, 2nw4, 3g0w – rAR + modulator
2hvc, 3b5r, 3b65, 3b66, 3b67, 3b68 – hAR + modulator

AR LBD domain complex with peptide

1t73, 1t74, 1t76, 1t79, 1t7f, 1t7m, 1t7r – cAR + FXXFF-type peptide
1xow – hAR + androgen + FXXFF-type peptide
2q7i – hAR + testosterone + FXXFF-type peptide
3v49, 3v4a – hAR + modulator + FXXFF-type peptide
1t5z – hAR + DHT + nuclear receptor coactivator 1 peptide
1t63, 1t65 – hAR + DHT + nuclear receptor coactivator 2 peptide
3l3x, 3l3z – hAR + DHT + nuclear receptor coactivator 3 peptide
2z4j – hAR + DHT + nuclear receptor 0B2 peptide
2q7j – hAR + testosterone + nuclear receptor coactivator 2 peptide
2q7k, 2q7l – hAR (mutant) + testosterone + nuclear receptor coactivator 2 peptide
2ao6 – hAR + nuclear receptor coactivator 2 peptide
1xj7 – hAR + DHT + RAC3 peptide