中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
首页 机构 成果 学者
  
  1. CAS IR Grid
  2. 上海药物研究所
  3. 中国科学院上海药物研究所
  4. 药物靶标结构与功能中心
热门
Androgen receptor: structure, role in prostate cancer and drug discovery

文献类型：期刊论文

作者Tan, M. H. Eileen2,3; Li, Jun2; Xu, H. Eric1,3; Melcher, Karsten3; Yong, Eu-leong2
刊名ACTA PHARMACOLOGICA SINICA
出版日期2015-01
卷号36期号:1页码:3-23
关键词androgen androgen receptor prostate cancer nuclear receptor drug discovery rational drug design structural biology castration resistance antiandrogen
ISSN号1671-4083
DOI10.1038/aps.2014.18
文献子类Review
英文摘要Androgens and androgen receptors (AR) play a pivotal role in expression of the male phenotype. Several diseases, such as androgen insensitivity syndrome (AIS) and prostate cancer, are associated with alterations in AR functions. Indeed, androgen blockade by drugs that prevent the production of androgens and/or block the action of the AR inhibits prostate cancer growth. However, resistance to these drugs often occurs after 2-3 years as the patients develop castration-resistant prostate cancer (CRPC). In CRPC, a functional AR remains a key regulator. Early studies focused on the functional domains of the AR and its crucial role in the pathology. The elucidation of the structures of the AR DNA binding domain (DBD) and ligand binding domain (LBD) provides a new framework for understanding the functions of this receptor and leads to the development of rational drug design for the treatment of prostate cancer. An overview of androgen receptor structure and activity, its actions in prostate cancer, and how structural information and high-throughput screening have been or can be used for drug discovery are provided herein.
WOS关键词LIGAND-BINDING DOMAIN ; STEROID-HORMONE RECEPTORS ; AMINO-TERMINAL DOMAIN ; ACTIVATION FUNCTION 2 ; HUMAN X-CHROMOSOME ; NUCLEAR RECEPTOR ; DNA-BINDING ; GENE-MUTATIONS ; TYROSINE PHOSPHORYLATION ; TRANSACTIVATION DOMAIN
资助项目Singapore National Medical Research Council[R-174-000-137-275] ; Jay and Betty Van Andel Foundation[00000000] ; Amway (China) Limited[00000000] ; National Institutes of Health[5R01DK071662-08] ; National Institutes of Health[GM102545] ; National Institutes of Health[GM104212] ; NUS Graduate School for Integrative Sciences Engineering[00000000]
WOS研究方向Chemistry ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000347389000002
出版者ACTA PHARMACOLOGICA SINICA
源URL[http://119.78.100.183/handle/2S10ELR8/276775]  
专题药物靶标结构与功能中心
通讯作者Tan, M. H. Eileen
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, VARI SIMM Ctr, Shanghai 201203, Peoples R China
2.Natl Univ Singapore, Yong Loo Lin Sch Med, Natl Univ Hosp, Dept Obstet & Gynecol, Singapore 117595, Singapore;
3.Van Andel Res Inst, Ctr Struct Biol & Drug Discovery, Lab Struct Sci, Grand Rapids, MI 49503 USA;
推荐引用方式
GB/T 7714		 Tan, M. H. Eileen,Li, Jun,Xu, H. Eric,et al. Androgen receptor: structure, role in prostate cancer and drug discovery[J]. ACTA PHARMACOLOGICA SINICA,2015,36(1):3-23.
APA Tan, M. H. Eileen,Li, Jun,Xu, H. Eric,Melcher, Karsten,&Yong, Eu-leong.(2015).Androgen receptor: structure, role in prostate cancer and drug discovery.ACTA PHARMACOLOGICA SINICA,36(1),3-23.
MLA Tan, M. H. Eileen,et al."Androgen receptor: structure, role in prostate cancer and drug discovery".ACTA PHARMACOLOGICA SINICA 36.1(2015):3-23.

入库方式： OAI收割

来源：上海药物研究所

浏览0
下载0
收藏0
其他版本

除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。