Androgen receptor
From Proteopedia
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| - | {{ | + | {{STRUCTURE_2hvc| PDB=2hvc | SIZE=350| SCENE= |right|CAPTION=Human androgen receptor ligand binding domain complex with testosterone and FXXFF-type peptide (green) and sulfate [[2q7i]] }} |
| - | '''Androgen receptor''' (AR) is a nuclear receptor which is activated by testosterone or 5-α-dihydrotestosterone (DHT) [[hormone]]. 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 structure is composed of 5 domains - <br /> | + | == Function == |
| - | A/B: N-terminal contains | + | |
| + | '''Androgen receptor''' (AR) is a nuclear receptor which is activated by testosterone or 5-α-dihydrotestosterone (DHT) [[hormone]]. 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. | ||
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| + | == Disease == | ||
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| + | Mutated AR is involved in male infertility and prostate cancer. In healthy people, one region of the AR gene shows upto 36 repeats of the CAG sequence. Patients with abnormally high number of CAG repeats can develop spinal muscular atrophy. | ||
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| + | == Structural highlights == | ||
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| + | AR structure is composed of 5 domains - <br /> | ||
| + | A/B: N-terminal regulatory domain contains activation function 1 (residues 101-370), activation function 5 (residues 360-485) and dimerization surface (residues 1-36 and 370-494).<br /> | ||
C: DNA binding domain (DBD)<br /> | C: DNA binding domain (DBD)<br /> | ||
D: Hinge region between DBD and LBD<br /> | D: Hinge region between DBD and LBD<br /> | ||
Revision as of 11:35, 1 November 2015
Contents |
Function
Androgen receptor (AR) is a nuclear receptor which is activated by testosterone or 5-α-dihydrotestosterone (DHT) hormone. 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.
Disease
Mutated AR is involved in male infertility and prostate cancer. In healthy people, one region of the AR gene shows upto 36 repeats of the CAG sequence. Patients with abnormally high number of CAG repeats can develop spinal muscular atrophy.
Structural highlights
AR structure is composed of 5 domains -
A/B: N-terminal regulatory domain contains activation function 1 (residues 101-370), activation function 5 (residues 360-485) and dimerization surface (residues 1-36 and 370-494).
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 01-November-2015
See Also
Proteopedia Page Contributors and Editors (what is this?)
Cristina Benito, Michal Harel, Cristina Murga, Marta Roldan Lazaro, Alexander Berchansky, Joel L. Sussman, Wayne Decatur, David Sánchez Fernández
