Androgen receptor: structure, role in prostate cancer and drug discovery

doi:10.1038/aps.2014.18

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药物靶标结构与功能中心

	Androgen receptor: structure, role in prostate cancer and drug discovery
	Tan, M. H. Eileen 2,3; Li, Jun2 ; Xu, H. Eric1,3 ; Melcher, Karsten 3; Yong, Eu-leong 2
刊名	ACTA PHARMACOLOGICA SINICA
	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
DOI	10.1038/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.
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
WOS研究方向	Chemistry ; Pharmacology & Pharmacy
语种	英语
出版者	ACTA PHARMACOLOGICA SINICA
WOS记录号	WOS:000347389000002
内容类型	期刊论文
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.