Cited by 1,780Prostate Cancer Treatment and ResearchEstrogen and related hormone effectsProstate Cancer Diagnosis and Treatment

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Androgen Receptor in Prostate Cancer

Heinlein, Cynthia A., Chang, Chawnshang·2004·Endocrine Reviews

DOI 10.1210/er.2002-0032

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Abstract

The normal development and maintenance of the prostate is dependent on androgen acting through the androgen receptor (AR). AR remains important in the development and progression of prostate cancer. AR expression is maintained throughout prostate cancer progression, and the majority of androgen-independent or hormone refractory prostate cancers express AR. Mutation of AR, especially mutations that result in a relaxation of AR ligand specificity, may contribute to the progression of prostate cancer and the failure of endocrine therapy by allowing AR transcriptional activation in response to antiandrogens or other endogenous hormones. Similarly, alterations in the relative expression of AR coregulators have been found to occur with prostate cancer progression and may contribute to differences in AR ligand specificity or transcriptional activity. Prostate cancer progression is also associated with increased growth factor production and an altered response to growth factors by prostate cancer cells. The kinase signal transduction cascades initiated by mitogenic growth factors modulate the transcriptional activity of AR and the interaction between AR and AR coactivators. The inhibition of AR activity through mechanisms in addition to androgen ablation, such as modulation of signal transduction pathways, may delay prostate cancer progression.

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Authors: Heinlein, C. A., & Chang, C.
Affiliations: University of Rochester Medicine (US)
ORCID: Chang, Chawnshang
Venue: Endocrine Reviews
Publisher: The Endocrine Society
Published: 2004-04-01
Volume: 25
Issue: 2
Pages: 276-308
ISSN: 0163-769X (ISSN-L)
1945-7189
DOI: 10.1210/er.2002-0032
OpenAlex: W2064293531
Cited by: 1,780
References: 419
Citations by year: 2026: 33 · 2025: 66 · 2024: 69 · 2023: 101 · 2022: 81 · 2021: 99 · 2020: 84 · 2019: 81 · 2018: 71 · 2017: 94 · 2016: 87 · 2015: 93 · 2014: 104 · 2013: 95 · 2012: 88
FWCI: 11.47
Type: journal article
Language: en
Open access: closed
Locations: Endocrine Reviews (publishedVersion)
PubMed (publishedVersion)
Funders: National Institute of Diabetes and Digestive and Kidney Diseases (DK 60948, R01DK060948, R01DK060905, DK60905)
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 › Urology › Prostate Cancer Diagnosis and Treatment
Keywords: androgen receptor, prostate cancer, castration-resistant prostate cancer, androgen receptor mutations, ligand specificity, growth factor signaling, endocrine therapy resistance, androgen deprivation therapy, prostate development
MeSH terms: Androgen Antagonists, Androgens, Animals, Cell Division, Growth Substances, Humans, Male, Mutation, Prostate, Prostatic Neoplasms, Receptors, Androgen, Repetitive Sequences, Nucleic Acid, Transcription, Genetic, Gene Expression, Genes, Tumor Suppressor, Apoptosis, Prostate-Specific Antigen

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Androgen Receptor in Prostate Cancer

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