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Androgen Receptor (AR) Coregulators: An Overview

Heinlein, Cynthia A., Chang, Chawnshang·2002·Endocrine Reviews

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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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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
DOI: 10.1210/edrv.23.2.0460
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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Androgen Receptor (AR) Coregulators: An Overview

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