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West Ashley Library
Closed for Staff Day
Phone: (843) 766-6635
Wando Mount Pleasant Library
Closed for Staff Day
Phone: (843) 805-6888
Village Library
Closed for Staff Day
Phone: (843) 884-9741
St. Paul's/Hollywood Library
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Phone: (843) 889-3300
Otranto Road Library
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Phone: (843) 572-4094
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Closed for Staff Day
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Main Library
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Targeting the N-Terminal Domain of the Androgen Receptor: A New Approach for the Treatment of Advanced Prostate Cancer.
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- Author(s): Antonarakis, Emmanuel S.; Chandhasin, Chandtip; Osbourne, Erica; Luo, Jun; Sadar, Marianne D.; Perabo, Frank
- Source:
Oncologist; Dec2016, Vol. 21 Issue 12, p1427-1435, 9p, 2 Diagrams, 1 Chart- Subject Terms:
- Source:
- Additional Information
- Abstract: Despite the recent approval and widespread use of abiraterone acetate and enzalutamide for the treatment of castration-resistant prostate cancer (CRPC), this disease still poses significant management challenges because of various tumor escape mechanisms, including those that allow androgen receptor (AR) signaling to remain active. These AR-related resistance mechanisms include AR gene amplification or over-expression, constitutively active ligand-independent AR splice variants, and gain-of-function mutations involving the AR ligand-binding domain (LBD), among others. Therefore, the development of AR-targeted therapies that function independently of the LBD represents an unmet medical need and has the potential to overcome many of these resistance mechanisms. This article discusses N-terminal domain (NTD) inhibition as a novel concept in the field of AR-directed therapies for prostate cancer. AR NTD-targeting agents have the potential to overcome shortcomings of current hormonal therapies by inhibiting all forms of AR-mediated transcriptional activity, and as a result, may affect a broader AR population including mutational and splice variant ARs. Indeed, the first clinical trial of an AR NTD inhibitor is now underway. [ABSTRACT FROM AUTHOR]
- Abstract: Copyright of Oncologist is the property of Oxford University Press / USA and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
- Abstract:
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