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Androgen receptor: structure, role in prostate cancer and drug discovery

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Tan, MH Eileen, Li, Jun, Xu, H Eric, Melcher, Karsten, Yong, Eu-leong·2015·Acta Pharmacologica Sinica
DOI 10.1038/aps.2014.18
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Abstract

Androgens and androgen receptors (AR) play a pivotal role in expression of the male phenotype. Several diseases, such as androgen insensitivity syndrome (AIS) and prostate cancer, are associated with alterations in AR functions. Indeed, androgen blockade by drugs that prevent the production of androgens and/or block the action of the AR inhibits prostate cancer growth. However, resistance to these drugs often occurs after 2-3 years as the patients develop castration-resistant prostate cancer (CRPC). In CRPC, a functional AR remains a key regulator. Early studies focused on the functional domains of the AR and its crucial role in the pathology. The elucidation of the structures of the AR DNA binding domain (DBD) and ligand binding domain (LBD) provides a new framework for understanding the functions of this receptor and leads to the development of rational drug design for the treatment of prostate cancer. An overview of androgen receptor structure and activity, its actions in prostate cancer, and how structural information and high-throughput screening have been or can be used for drug discovery are provided herein.

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Cited by

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Metadata

Authors
Tan, M. E., Li, J., Xu, H. E., Melcher, K., & Yong, E.-L.
Venue
Acta Pharmacologica Sinica
Publisher
Springer Science and Business Media LLC
Published
2014-06-09
Volume
36
Issue
1
Pages
3-23
ISSN
  • 0253-9756 (ISSN-L)
  • 1671-4083
  • 1745-7254
DOI
10.1038/aps.2014.18
OpenAlex
W1968786809
Cited by
943
References
29
FWCI
25.69
Type
journal article
Language
en
Open access
hybrid
Licence
creativecommons.org/licenses/by-nc-nd/3.0 (tdm)

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CoChat. (2026). Citation check: Androgen receptor: structure, role in prostate cancer and drug discovery. https://app.cochat.ai/papers/10.1038/aps.2014.18
The paper
Tan, M. E., Li, J., Xu, H. E., Melcher, K., & Yong, E.-L. (2015). Androgen receptor: structure, role in prostate cancer and drug discovery. Acta Pharmacologica Sinica. https://doi.org/10.1038/aps.2014.18

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

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