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Androgen Receptor (AR) Coregulators: An Overview
Abstract
The biological action of androgens is mediated through the androgen receptor (AR). Androgen-bound AR functions as a transcription factor to regulate genes involved in an array of physiological processes, most notably male sexual differentiation and maturation, and the maintenance of spermatogenesis. The transcriptional activity of AR is affected by coregulators that influence a number of functional properties of AR, including ligand selectivity and DNA binding capacity. As the promoter of target genes, coregulators participate in DNA modification, either directly through modification of histones or indirectly by the recruitment of chromatin-modifying complexes, as well as functioning in the recruitment of the basal transcriptional machinery. Aberrant coregulator activity due to mutation or altered expression levels may be a contributing factor in the progression of diseases related to AR activity, such as prostate cancer. AR demonstrates distinct differences in its interaction with coregulators from other steroid receptors due to differences in the functional interaction between AR domains, possibly resulting in alterations in the dynamic interactions between coregulator complexes.
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“Androgen receptors can be modulated by specific proteins called coregulators [70–72] or mediated via the activation of membrane-bound protein receptors to initiate intracellular signalling pathways [73], which can occur even in the presence of low levels of androgens [74].”
From Integrating Transwomen and Female Athletes with Differences of Sex Development (DSD) into Elite Competition: The FIMS 2021 Consensus Statement (2021) · cites this paper as [70]
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Metadata
- Authors
- Heinlein, C. A., & Chang, C.
- Affiliations
- University of Rochester Medicine (US)
- Corresponding author
- Chang, Chawnshang
- ORCID
- Chang, Chawnshang
- Venue
- Endocrine Reviews
- Publisher
- The Endocrine Society
- Published
- 2002-04-01
- Volume
- 23
- Issue
- 2
- Pages
- 175-200
- ISSN
- 0163-769X (ISSN-L)
- 1945-7189
- OpenAlex
- W2161123101
- Cited by
- 943
- References
- 357
- Citations by year
- 2026: 13 · 2025: 18 · 2024: 28 · 2023: 22 · 2022: 30 · 2021: 19 · 2020: 26 · 2019: 25 · 2018: 23 · 2017: 30 · 2016: 32 · 2015: 48 · 2014: 34 · 2013: 48 · 2012: 44
- FWCI
- 12.87
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Endocrine Reviews (publishedVersion)
- PubMed (publishedVersion)
- Funders
- University of Rochester
- National Institutes of Health (14642)
- Medical Center, University of Rochester
- National Cancer Institute (CA55639, CA-715670)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Prostate Cancer Treatment and Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
- Health Sciences › Medicine › Reproductive Medicine › Sperm and Testicular Function
- Keywords
- androgen receptor, coregulators, transcriptional regulation, androgen signaling, histone modifications, chromatin remodeling, basal transcription machinery, ligand selectivity, DNA binding, prostate cancer, steroid hormone receptors, male sexual differentiation, spermatogenesis
- MeSH terms
- Animals, Gene Expression Regulation, Humans, Male, Mutation, Prostatic Neoplasms, Receptors, Androgen, Transcription Factors, Transcription, Genetic, Signal Transduction
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