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Molecular Biology of the Androgen Receptor

Gelmann, Edward P.·2002·Journal of Clinical Oncology
DOI 10.1200/jco.2002.10.018
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Abstract

ABSTRACT: Androgen receptor (AR) is a member of the steroid hormone receptor family of molecules. AR primarily is responsible for mediating the physiologic effects of androgens by binding to specific DNA sequences that influence transcription of androgen-responsive genes. The three-dimensional structure of the AR ligand-binding domain has shown it is similar to other steroid hormone receptors and that ligand binding alters the protein conformation to allow binding of coactivator molecules that amplify the hormone signal and mediate transcriptional initiation. However, AR also undergoes intramolecular interactions that regulate its interactions with coactivators and influence its activity. A large number of naturally occurring mutations of the human AR gene have provided important information about AR molecular structure and intermolecular interactions. AR is also a critical mediator of prostate cancer promotion, conferring growth signals to prostate cancer cells throughout the natural history of the disease. Late-stage prostate cancer, unresponsive to hormonal deprivation, sustains AR signaling through a diverse array of molecular strategies. Variations in the AR gene may also confer genetic predisposition to prostate cancer development and severity. Further understanding of AR action and new strategies to interfere with AR signaling hold promise for improving prostate cancer therapy.

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Metadata

Authors
Gelmann, E. P.
Venue
Journal of Clinical Oncology
Publisher
American Society of Clinical Oncology (ASCO)
Published
2002-07-01
Volume
20
Issue
13
Pages
3001-3015
ISSN
  • 0732-183X (ISSN-L)
  • 1527-7755
DOI
10.1200/jco.2002.10.018
OpenAlex
W2125069527
Cited by
942
References
7
FWCI
34.16
Type
journal article
Language
en
Open access
closed

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Gelmann, E. P. (2002). Molecular Biology of the Androgen Receptor. Journal of Clinical Oncology. https://doi.org/10.1200/jco.2002.10.018

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