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AR-V7 and Resistance to Enzalutamide and Abiraterone in Prostate Cancer

by Roeser, Jeffrey C , De Marzo, Angelo M , Antonarakis, Emmanuel S , Isaacs, John T , Luber, Brandon , Mohammad, Tabrez A , Chen, Yan , Chen, Yidong , Isaacs, William B , Denmeade, Samuel R , Luo, Jun , Lotan, Tamara L , Zheng, Qizhi , Nadal, Rosa , Fedor, Helen L , Eisenberger, Mario A , Carducci, Michael A , Paller, Channing J , Nakazawa, Mary , Lu, Changxue , Wang, Hao

in Alternative splicing / Androgen receptors / Androgens / Androstenes / Androstenols - therapeutic use / Biological and medical sciences / Cancer therapies / Castration / Drug resistance / Drug Resistance, Neoplasm - genetics / General aspects / Gynecology. Andrology. Obstetrics / Humans / Ligands / Male / Male genital diseases / Medical sciences / Metastases / Metastasis / Morphinans - analysis / mRNA / Nephrology. Urinary tract diseases / Patients / Phenylthiohydantoin - analogs & derivatives / Phenylthiohydantoin - therapeutic use / Prostate cancer / Prostate-specific antigen / Prostatic Neoplasms - drug therapy / Prostatic Neoplasms - genetics / Proteins / Receptors, Androgen - analysis / Receptors, Androgen - genetics / Reverse Transcriptase Polymerase Chain Reaction / RNA, Neoplasm - analysis / Survival Analysis / Tumor cells / Tumors / Tumors of the urinary system / Urinary tract. Prostate gland

2014

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AR-V7 and Resistance to Enzalutamide and Abiraterone in Prostate Cancer

2014

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2014

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Journal Article

AR-V7 and Resistance to Enzalutamide and Abiraterone in Prostate Cancer

Roeser, Jeffrey C,

De Marzo, Angelo M,

Antonarakis, Emmanuel S,

Isaacs, John T,

Luber, Brandon,

Mohammad, Tabrez A,

Chen, Yan,

Chen, Yidong,

Isaacs, William B,

Denmeade, Samuel R,

Luo, Jun,

Lotan, Tamara L,

Zheng, Qizhi,

Nadal, Rosa,

Fedor, Helen L,

Eisenberger, Mario A,

Carducci, Michael A,

Paller, Channing J,

Nakazawa, Mary,

Lu, Changxue,

Wang, Hao

2014

Overview

Enzalutamide and abiraterone target the androgen receptor and androgen synthesis and are used to treat castration-resistant prostate cancer. A splice variant of the androgen receptor is associated with resistance to both drugs. It is now accepted that castration-resistant prostate cancer is not androgen-independent and continues to rely on androgen signaling. 1 Owing to this new understanding, several drugs have recently emerged for the treatment of castration-resistant prostate cancer; these agents either suppress the synthesis of extragonadal androgens or target the androgen receptor directly. 2 Enzalutamide is an inhibitor of androgen-receptor signaling that exerts its activity by binding avidly to the ligand-binding domain of the androgen receptor, competing with and displacing the natural ligands of this receptor (testosterone and dihydrotestosterone) while also inhibiting translocation of the androgen receptor into the nucleus and impairing transcriptional activation . . .

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Publisher

Massachusetts Medical Society

Subject

/ Androstenols - therapeutic use

/ Biological and medical sciences

/ Cancer therapies