Androgen receptor: Difference between revisions
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Two transcriptional activation functions have been identified: | Two transcriptional activation functions have been identified: | ||
*The ligand-independent AF-1 (residues 142-485): located in the NTD is constitutively active. It is the main region responsible for mediating AR transcription. Its contains two separable transcription activation units that are indispensable for full activity of the AR <ref name="Structure" />. | *The ligand-independent AF-1 (residues 142-485): located in the NTD is constitutively active. It is the main region responsible for mediating AR transcription. Its contains two separable transcription activation units that are indispensable for full activity of the AR <ref name="Structure" />. | ||
*The ligand-dependent AF-2: is located in the LBD <ref name="Bench to Bedside" />. <scene name='54/543362/H12_androgen_receptor/1'>Helix 12 (H12)</scene> forms the core of this region and acts as a lid to close the | *The ligand-dependent AF-2: is located in the LBD <ref name="Bench to Bedside" />. <scene name='54/543362/H12_androgen_receptor/1'>Helix 12 (H12)</scene> forms the core of this region and acts as a lid to close the LBD upon agonist binding <ref name="Structure" />. It is important for forming the coregulator bindings site as well as mediating direct interactions between the N-terminal and LBD. Key differences in the contribution of specific conserved residues in the AF-2 core domain between the AR and other steroid hormone nuclear receptors have been identified, it would explain the differences in the structure and the function, as well as the coregulatory proteins they interact with <ref name="Bench to Bedside" />. | ||
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==AR signaling== | ==AR signaling== | ||
AR has two mechanisms of action: the DNA binding-dependent (genomic AR signaling) and the DNA binding independent (non-genomic AR signaling). | AR has two mechanisms of action: the DNA binding-dependent (genomic AR signaling) and the DNA binding independent (non-genomic AR signaling). | ||
'''[[Image:MoA.jpg | thumb | centre | upright=3.0]]''' | '''[[Image:MoA.jpg | thumb | centre | upright=3.0 | Reproduced from Davey & Grossmann. <ref name="Bench to Bedside" />]]''' | ||
===DNA-Binding dependent actions of the AR=== | ===DNA-Binding dependent actions of the AR=== | ||
