An ultra-HTS process for the identification of small molecule modulators of orphan G-protein-coupled receptors

被引:27
作者
Cacace, A
Banks, M
Spicer, T
Civoli, F
Watson, J
机构
[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Lead Discovery, Wallingford, CT 06492 USA
[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Discovery Technol, Wallingford, CT 06492 USA
[3] Clin Immunol Amgen, Thousand Oaks, CA 91320 USA
关键词
D O I
10.1016/S1359-6446(03)02809-5
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
G-protein-coupled receptors (GPCRs) are the most successful target proteins for drug discovery research to date. More than 150 orphan GPCRs of potential therapeutic interest have been identified for which no activating ligands or biological functions are known. One of the greatest challenges in the pharmaceutical industry is to link these orphan GPCRs with human diseases. Highly automated parallel approaches that integrate ultra-high throughput and focused screening can be used to identify small molecule modulators of orphan GPCRs. These small molecules can then be employed as pharmacological tools to explore the function of orphan receptors in models of human disease, In this review, we describe methods that utilize powerful ultra-high-through put screening technologies to identify surrogate ligands of orphan GPCRs.
引用
收藏
页码:785 / 792
页数:8
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