Integrating the discovery pipeline for novel compounds targeting ion channels.
Integrating the discovery pipeline for novel compounds targeting ion channels.
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DOI：
10.1016/j.cbpa.2008.07.012
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发表时间：
2008-08
影响因子：
7.8
通讯作者：
Bulaj, Grzegorz
中科院分区：
文献类型：
--
作者：
Bulaj, Grzegorz
许多离子通道是治疗神经或心血管疾病的有吸引力的治疗靶点；对选择性通道拮抗剂和/或激动剂的需求持续存在。最近，已经开发了几项技术，使探索毒液来源的多肽毒素的巨大多样性变得更加可行。外基因组学与合成方法如二硒或氟桥、主链间隔基和N-到-C环化的结合提供了一种新兴技术，有望加速基于天然产物的化合物的发现和开发。与这些药物发现工作相辅相成的是调节离子通道和受体活动的新方法。综上所述，这些技术将促进我们对离子通道的了解和理解，并将加速它们作为一流治疗靶点的扩展。
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.
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影响因子：
14.8
作者：
Donia, Mohamed S.;Hathaway, Brian J.;Schmidt, Eric W.
通讯作者：
Schmidt, Eric W.
DOI：
10.1073/pnas.0504613102
发表时间：
2005-09-27
影响因子：
11.1
作者：
Clark, RJ;Fischer, H;Craik, DJ
通讯作者：
Craik, DJ
DOI：
10.1016/j.bbrc.2007.06.138
发表时间：
2007-09-14
影响因子：
3.1
作者：
Blanchfield, Joanne T.;Gallagher, Oliver P.;Toth, Istvan
通讯作者：
Toth, Istvan
影响因子：
14.8
作者：
Donia, Mohamed S.;Ravel, Jacques;Schmidt, Eric W.
通讯作者：
Schmidt, Eric W.
影响因子：
4.8
作者：
Armishaw, Christopher J.;Daly, Norelle L.;Alewood, Paul F.
通讯作者：
Alewood, Paul F.