Molecular mechanisms of androgen receptor-mediated gene regulation: structure-function analysis of the AF-1 domain

McEwan, I J

doi:10.1677/erc.0.0110281

Cited by 156Prostate Cancer Treatment and ResearchEstrogen and related hormone effectsGenomics and Chromatin Dynamics

Molecular mechanisms of androgen receptor-mediated gene regulation: structure-function analysis of the AF-1 domain

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McEwan, I J·2004·Endocrine-related cancer

DOI 10.1677/erc.0.0110281

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Abstract

The androgen receptor is a ligand-activated transcription factor that binds DNA response elements as a homodimer. Binding sites for the receptor have been identified both upstream and downstream of the transcription start site. Once bound to DNA, the receptor contacts chromatin remodelling complexes, coactivator proteins and components of the general transcription machinery in order to regulate target gene expression. The main transactivation domain, termed AF1, is located within the structurally distinct amino-terminal domain. This region is structurally flexible but adopts a more folded conformation in the presence of the binding partner TFIIF, and this in turn enhances subsequent protein-protein interactions. Thus, there is likely to be a dynamic interplay between protein-protein interactions and protein folding, involving AF1, that is proposed to lead to the assembly and/or disassembly of receptor-dependent transcription complexes.

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AR AF-1 is responsible for p300 recruitment because the majority of the AR-Ab1 binding region is AF-1 (amino acids 142-485).
“This suggests that AR AF-1 is responsible for p300 recruitment since majority of AR-Ab1 binding region is the AF-1 (aa 142–485) (McEwan, 2004).”
From Structural Insights of Transcriptionally Active, Full-Length Androgen Receptor Coactivator Complexes (2020) · cites this paper as McEwan, 2004
The Transcriptional activation section defines AR AF-1 as amino acids 142–485. The Protein-protein interactions section reports that AR acetylation enhances p300 binding, but it does not identify an AR-Ab1 binding region or establish that AF-1 is responsible for p300 recruitment. Page numbers are unavailable in our copy. (LLM, conf=0.83)
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Authors: McEwan, I. J.
Affiliations: University of Aberdeen (GB)
Corresponding author: McEwan, I J
ORCID: McEwan, I J
Venue: Endocrine-related cancer
Publisher: Bioscientifica
Published: 2004-06-01
Volume: 11
Issue: 2
Pages: 281-293
ISSN: 1351-0088 (ISSN-L)
1479-6821
DOI: 10.1677/erc.0.0110281
OpenAlex: W2170954128
Cited by: 156
References: 115
Citations by year: 2026: 1 · 2025: 6 · 2024: 4 · 2023: 3 · 2022: 5 · 2021: 2 · 2020: 5 · 2019: 6 · 2018: 9 · 2017: 8 · 2016: 5 · 2015: 9 · 2014: 5 · 2013: 7 · 2012: 13
FWCI: 1.74
Type: journal article
Language: en
Open access: bronze
doi.org
Locations: Endocrine Related Cancer (publishedVersion)
PubMed (publishedVersion)
Funders: University of Aberdeen
Directorate for Biological Sciences
Medical Research Council
Topics: Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Prostate Cancer Treatment and Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Genomics and Chromatin Dynamics
Keywords: androgen receptor, transcriptional activation, protein-protein interaction, TFIIF, protein folding, chromatin remodeling, transcriptional coactivator, general transcription machinery, ligand-activated transcription factors, gene expression regulation
MeSH terms: Gene Expression Regulation, Humans, Receptors, Androgen, Transcriptional Activation, Transcription Factors, TFII, Protein Interaction Mapping

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Molecular mechanisms of androgen receptor-mediated gene regulation: structure-function analysis of the AF-1 domain

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