Posttranslational regulation of androgen dependent and independent androgen receptor activities in prostate cancer

Prostate cancer (PCa) is the most commonly diagnosed cancer among men in western countries. Androgen receptor (AR) signaling plays key roles in the development of PCa. Androgen deprivation therapy (ADT) remains the standard therapy for advanced PCa. In addition to its ligand androgen, accumulating e...

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Main Authors: Simeng Wen, Yuanjie Niu, Haojie Huang
Format: Article
Language:English
Published: Elsevier 2020-07-01
Series:Asian Journal of Urology
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Online Access:http://www.sciencedirect.com/science/article/pii/S2214388219301110
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author Simeng Wen
Yuanjie Niu
Haojie Huang
author_facet Simeng Wen
Yuanjie Niu
Haojie Huang
author_sort Simeng Wen
collection DOAJ
description Prostate cancer (PCa) is the most commonly diagnosed cancer among men in western countries. Androgen receptor (AR) signaling plays key roles in the development of PCa. Androgen deprivation therapy (ADT) remains the standard therapy for advanced PCa. In addition to its ligand androgen, accumulating evidence indicates that posttranscriptional modification is another important mechanism to regulate AR activities during the progression of PCa, especially in castration resistant prostate cancer (CRPC). To date, a number of posttranscriptional modifications of AR have been identified, including phosphorylation (e.g. by CDK1), acetylation (e.g. by p300 and recognized by BRD4), methylation (e.g. by EZH2), ubiquitination (e.g. by SPOP), and SUMOylation (e.g. by PIAS1). These modifications are essential for the maintenance of protein stability, nuclear localization and transcriptional activity of AR. This review summarizes posttranslational modifications that influence androgen-dependent and -independent activities of AR, PCa progression and therapy resistance. We further emphasize that in addition to androgen, posttranslational modification is another important way to regulate AR activity, suggesting that targeting AR posttranslational modifications, such as proteolysis targeting chimeras (PROTACs) of AR, represents a potential and promising alternate for effective treatment of CRPC. Potential areas to be investigated in the future in the field of AR posttranslational modifications are also discussed.
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spelling doaj-art-b09eec14e67c414cbea5416730ba8a0c2025-08-20T03:04:29ZengElsevierAsian Journal of Urology2214-38822020-07-017320321810.1016/j.ajur.2019.11.001Posttranslational regulation of androgen dependent and independent androgen receptor activities in prostate cancerSimeng Wen0Yuanjie Niu1Haojie Huang2Department of Urology, The Second Hospital of Tianjin Medical University, Tianjin Institute of Urology, Tianjin Medical University, Tianjin, China; Department of Biochemistry and Molecular Biology, Mayo Clinic College of Medicine and Science, Rochester, USADepartment of Urology, The Second Hospital of Tianjin Medical University, Tianjin Institute of Urology, Tianjin Medical University, Tianjin, China; Corresponding author.Department of Biochemistry and Molecular Biology, Mayo Clinic College of Medicine and Science, Rochester, USA; Department of Urology, Mayo Clinic College of Medicine and Science, Rochester, USA; Mayo Clinic Cancer Center, Mayo Clinic College of Medicine and Science, Rochester, USA; Corresponding author. Department of Biochemistry and Molecular Biology, Mayo Clinic College of Medicine and Science, Rochester, USA.Prostate cancer (PCa) is the most commonly diagnosed cancer among men in western countries. Androgen receptor (AR) signaling plays key roles in the development of PCa. Androgen deprivation therapy (ADT) remains the standard therapy for advanced PCa. In addition to its ligand androgen, accumulating evidence indicates that posttranscriptional modification is another important mechanism to regulate AR activities during the progression of PCa, especially in castration resistant prostate cancer (CRPC). To date, a number of posttranscriptional modifications of AR have been identified, including phosphorylation (e.g. by CDK1), acetylation (e.g. by p300 and recognized by BRD4), methylation (e.g. by EZH2), ubiquitination (e.g. by SPOP), and SUMOylation (e.g. by PIAS1). These modifications are essential for the maintenance of protein stability, nuclear localization and transcriptional activity of AR. This review summarizes posttranslational modifications that influence androgen-dependent and -independent activities of AR, PCa progression and therapy resistance. We further emphasize that in addition to androgen, posttranslational modification is another important way to regulate AR activity, suggesting that targeting AR posttranslational modifications, such as proteolysis targeting chimeras (PROTACs) of AR, represents a potential and promising alternate for effective treatment of CRPC. Potential areas to be investigated in the future in the field of AR posttranslational modifications are also discussed.http://www.sciencedirect.com/science/article/pii/S2214388219301110Androgen receptorPosttranslational modificationPhosphorylationAcetylationMethylationUbiquitination
spellingShingle Simeng Wen
Yuanjie Niu
Haojie Huang
Posttranslational regulation of androgen dependent and independent androgen receptor activities in prostate cancer
Asian Journal of Urology
Androgen receptor
Posttranslational modification
Phosphorylation
Acetylation
Methylation
Ubiquitination
title Posttranslational regulation of androgen dependent and independent androgen receptor activities in prostate cancer
title_full Posttranslational regulation of androgen dependent and independent androgen receptor activities in prostate cancer
title_fullStr Posttranslational regulation of androgen dependent and independent androgen receptor activities in prostate cancer
title_full_unstemmed Posttranslational regulation of androgen dependent and independent androgen receptor activities in prostate cancer
title_short Posttranslational regulation of androgen dependent and independent androgen receptor activities in prostate cancer
title_sort posttranslational regulation of androgen dependent and independent androgen receptor activities in prostate cancer
topic Androgen receptor
Posttranslational modification
Phosphorylation
Acetylation
Methylation
Ubiquitination
url http://www.sciencedirect.com/science/article/pii/S2214388219301110
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AT yuanjieniu posttranslationalregulationofandrogendependentandindependentandrogenreceptoractivitiesinprostatecancer
AT haojiehuang posttranslationalregulationofandrogendependentandindependentandrogenreceptoractivitiesinprostatecancer