Integrating the discovery pipeline for novel compounds targeting ion channels

被引:22
作者
Bulaj, Grzegorz [1 ]
机构
[1] Univ Utah, Dept Med Chem, Coll Pharm, Salt Lake City, UT 84108 USA
关键词
D O I
10.1016/j.cbpa.2008.07.012
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Many ion channels are attractive therapeutic targets for the treatment of neurological or cardiovascular diseases; there is a continuous need for selective channel antagonists and/or agonists. Recently, several technologies have been developed that make exploration of the enormous diversity of venom-derived peptidic toxins more feasible. Integration of exogenomics with synthetic methods such as diselenide or fluorous bridges, backbone spacers, and N-to-C cyclization provides an emerging technology that promises to accelerate discovery and development of natural products based compounds. These drug-discovery efforts are complemented by novel approaches to modulate the activities of ion channels and receptors. Taken together, these technologies will advance our knowledge and understanding of ion channels and will accelerate their expansion as targets for first-in-class therapeutics.
引用
收藏
页码:441 / 447
页数:7
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