New insights into the androgen biotransformation in prostate cancer: A regulatory network among androgen, androgen receptors and UGTs

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• 作者：Xuan Qin^a ; Mingyao Liu^a ; ^b ; Xin Wang^a ; ^{usxinwang@gmail.com" class="auth_mail" title="E-mail the corresponding author} ; ^{xwang@bio.ecnu.edu.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Bicalutamide (PubChem CID ; 2375) ; Flutamide (PubChem CID ; 3397) ; Enzalutamide (PubChem CID ; 15951529) ; Abiraterone acetate (PubChem CID ; 57336518) ; Finasteride (PubChem CID ; 57363) ; Dutasteride (PubChem CID ; 6918296) ; Dihydrotestosterone (PubChem CID ; 10635) ; Testosterone (PubChem CID ; 6013) ; Androsterone (PubChem CID ; 5879) ; Dehydroepiandrosterone (PubChem CID ; 5881) ; Orteronel (PubChem CID ; 9796590)
• 刊名：Pharmacological Research
• 出版年：2016
• 出版时间：April 2016
• 年：2016
• 卷：106
• 期：Complete
• 页码：114-122
• 全文大小：1498 K

文摘

Androgen, as one kind of steroid hormones, is pivotal in the hormone-sensitive cancer, such as prostate cancer (PCa). The synthesis, elimination, and bioavailability of androgen in prostate cells have been proved to be a main cause of the carcinogenesis, maintenance and deterioration of PCa. This review illustrates the outlines of androgen biotransformation, and further discusses the different enzymes, especially UDP-glucuronyltransferases (UGTs) embedded in both benign and malignant prostate cells, which catalyze the reactions. Although many inhibitors of the enzymes responsible for the synthesis of androgens have been developed into drugs to fight against PCa, the elimination procedures metabolized by the UGTs are less emphasized. Thus the regulatory network among androgen, androgen receptors (AR) and UGTs is carefully reviewed in this article, indicating the determinant effects of UGTs on prostatic androgens and the regulation of AR. Finally, the hypothesis is also put forward that the regulators of UGTs may be developed to accelerate the androgen elimination and benefit PCa therapy.