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治疗性雄激素受体配体

Therapeutic androgen receptor ligands.

作者信息

Allan George F, Sui Zhihua

机构信息

Johnson and Johnson Pharmaceutical Research and Development, Department of Reproductive Therapeutics, Raritan, NJ 08869, USA.

出版信息

Nucl Recept Signal. 2003;1:e009. doi: 10.1621/nrs.01009. Epub 2003 Sep 27.

DOI:10.1621/nrs.01009
PMID:16604181
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1402218/
Abstract

In the past several years, the concept of tissue-selective nuclear receptor ligands has emerged. This concept has come to fruition with estrogens, with the successful marketing of drugs such as raloxifene. The discovery of raloxifene and other selective estrogen receptor modulators (SERMs) has raised the possibility of generating selective compounds for other pathways, including androgens (that is, selective androgen receptor modulators, or SARMs).

摘要

在过去几年中，组织选择性核受体配体的概念应运而生。随着雷洛昔芬等药物的成功上市，这一概念在雌激素领域得以实现。雷洛昔芬及其他选择性雌激素受体调节剂（SERM）的发现，增加了开发针对其他信号通路（包括雄激素，即选择性雄激素受体调节剂，或SARM）的选择性化合物的可能性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6818/1402218/30b5560fb760/nrs01009.f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6818/1402218/d872ea2b7199/nrs01009.f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6818/1402218/94d6646b8a0b/nrs01009.f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6818/1402218/4ec2691d21ba/nrs01009.f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6818/1402218/30b5560fb760/nrs01009.f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6818/1402218/d872ea2b7199/nrs01009.f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6818/1402218/94d6646b8a0b/nrs01009.f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6818/1402218/4ec2691d21ba/nrs01009.f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6818/1402218/30b5560fb760/nrs01009.f4.jpg

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本文引用的文献

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Clin Endocrinol (Oxf). 2002 Aug;57(2):231-4. doi: 10.1046/j.1365-2265.2002.01594.x.
2
Bicalutamide as immediate therapy either alone or as adjuvant to standard care of patients with localized or locally advanced prostate cancer: first analysis of the early prostate cancer program.比卡鲁胺作为局限性或局部晚期前列腺癌患者的即时单一治疗或标准治疗辅助用药：早期前列腺癌项目的首次分析
J Urol. 2002 Aug;168(2):429-35.
3
Androgen deficiency in the aging male: pathophysiology, diagnosis, and treatment alternatives.
Pharm Res. 2006 Aug;23(8):1641-58. doi: 10.1007/s11095-006-9024-3.
4
Comparison of the pharmacological effects of a novel selective androgen receptor modulator, the 5alpha-reductase inhibitor finasteride, and the antiandrogen hydroxyflutamide in intact rats: new approach for benign prostate hyperplasia.新型选择性雄激素受体调节剂、5α-还原酶抑制剂非那雄胺及抗雄激素药物羟基氟他胺在成年大鼠体内的药理作用比较：良性前列腺增生的新研究方法
Endocrinology. 2004 Dec;145(12):5420-8. doi: 10.1210/en.2004-0627. Epub 2004 Aug 12.
老年男性雄激素缺乏：病理生理学、诊断及治疗选择
Curr Urol Rep. 2001 Dec;2(6):473-9. doi: 10.1007/s11934-001-0042-8.
4
Androgen receptor (AR) coregulators: an overview.雄激素受体（AR）共调节因子：概述
Endocr Rev. 2002 Apr;23(2):175-200. doi: 10.1210/edrv.23.2.0460.
5
New alternative treatment in hirsutism: bicalutamide 25 mg/day.多毛症的新型替代疗法：比卡鲁胺，每日25毫克。
Gynecol Endocrinol. 2002 Feb;16(1):63-6.
6
Low-dose flutamide (125 mg/day) as maintenance therapy in the treatment of hirsutism.
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7
Crystallographic structures of the ligand-binding domains of the androgen receptor and its T877A mutant complexed with the natural agonist dihydrotestosterone.雄激素受体及其T877A突变体与天然激动剂二氢睾酮复合的配体结合域的晶体结构。
Proc Natl Acad Sci U S A. 2001 Apr 24;98(9):4904-9. doi: 10.1073/pnas.081565498.
8
Gynecomastia in patients with prostate cancer: a review of treatment options.
Urology. 2000 Nov 1;56(5):713-20. doi: 10.1016/s0090-4295(00)00823-2.
9
Structural evidence for ligand specificity in the binding domain of the human androgen receptor. Implications for pathogenic gene mutations.人类雄激素受体结合域中配体特异性的结构证据。对致病基因突变的影响。
J Biol Chem. 2000 Aug 25;275(34):26164-71. doi: 10.1074/jbc.M004571200.
10
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Int J Pharm. 2000 Jan 20;194(1):125-34. doi: 10.1016/s0378-5173(99)00359-2.