摘要
雄性激素和雄激素受体(AR)在前列腺癌的发展中起着至关重要的作用。雄激素阻断疗法(ADT)已经成为治疗转移性前列腺癌患者的主要方法。ADT能够降低血清睾酮水平,从正常范围500到600ng/dl之间到切除睾丸后的水平。手术切除睾丸后,大约四分之三的病人的血清睾酮水平降到不足20ng/dl(0.69nmol/L)。虽然在进行ADT后导致血清睾酮水平的抑制不足到目前为止仍未被充分认识到,但是在切除睾丸后的睾丸素水平降低的不成功对前列腺癌证幸存患者确实产生了副作用。尽管在去除睾丸后的循环的睾丸素水平不一定反映前列腺内睾丸素或者二氢睾酮,睾丸素的数量,ADT治疗主要源自于瘤内合成前体细胞和肾上腺雄激素。以分别针对肾上腺或者前列腺内雄性激素的生物合成的醋酸阿比特龙和针对增强AR信号的恩咋鲁胺为代表的新兴药物已经恢复了在ADT过程中的睾丸素水平的热度。我们用专门对雄性激素代谢和其在前列腺癌生物学和治疗方面的重大意义进行了综述,以促进对它们更好的了解及其在前列腺癌患者中更好的作用。
关键词: 雄性激素代谢,雄激素受体,雄激素阻断治疗,前列腺癌
图形摘要
Current Drug Targets
Title:Androgen Metabolic Pathway Involved in Current and Emerging Treatment for Men with Castration Resistant Prostate Cancer: Intraprostatic Androgens as Therapeutic Targets and Endocrinological Biomarkers
Volume: 15 Issue: 13
Author(s): Noboru Hara and Noboru Hara
Affiliation:
关键词: 雄性激素代谢,雄激素受体,雄激素阻断治疗,前列腺癌
摘要: Androgen and androgen receptor (AR) play a critical role in the development of prostate cancer. Androgen deprivation therapy (ADT) has become the therapeutic mainstay for patients with metastatic prostate cancer. ADT can reduce the serum testosterone level from the normal range between 500 and 600 ng/dl to the castrate level. Following surgical castration, the serum testosterone level decreases to less than 20 ng/dL (0.69 nmol/L) in about three quarters of the patients. Although insufficient suppressions of the serum testosterone level following ADT have not been well recognized to date, the failure in achieving the castrate level of testosterone may have an adverse impact on survival in men with prostate cancer. Although circulating testosterone levels following castration do not necessarily reflect the amount of intraprostatic testosterone or dihydrotestosterone, testosterone during ADT mainly derives from intratumorally synthesized precursors and adrenal androgens. The advent of new agents represented by abiraterone acetate and enzalutamide, which target adrenal or intraprostatic androgen biosynthesis and AR signaling, respectively, has retrieved interest in testosterone levels during ADT. We critically reviewed androgen metabolism and its significance in prostate cancer biology and treatment to promote their better understanding and management of men with prostate cancer.
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Noboru Hara and Hara Noboru, Androgen Metabolic Pathway Involved in Current and Emerging Treatment for Men with Castration Resistant Prostate Cancer: Intraprostatic Androgens as Therapeutic Targets and Endocrinological Biomarkers, Current Drug Targets 2014; 15 (13) . https://dx.doi.org/10.2174/1389450115666141024114736
DOI https://dx.doi.org/10.2174/1389450115666141024114736 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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