Synthesis and evaluation of hermitamides A and B as human voltage-gated sodium channel blockers.
Synthesis and evaluation of hermitamides A and B as human voltage-gated sodium channel blockers.
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DOI：
10.1016/j.bmc.2011.05.043
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发表时间：
2011-07-15
影响因子：
3.5
通讯作者：
Paige, Mikell
中科院分区：
文献类型：
--
作者：
De Oliveira, Eliseu O.;Graf, Kristin M.;Patel, Manoj K.;Baheti, Aparna;Kong, Hye-Sik;MacArthur, Linda H.;Dakshanamurthy, Sivanesan;Wang, Kan;Brown, Milton L.;Paige, Mikell
Hermitamides A and B are lipopeptides isolated from a Papau New Guinea collection of the marine cyanobacterium Lyngbya majuscula. We hypothesized that the hermitamides are ligands for the human voltage-gated sodium channel (hNaV) based on their structural similarity to the jamaicamides. Herein, we describe the nonracemic total synthesis of hermitamides A and B and their epimers. We report the ability of the hermitamides to displace [3H]-BTX at 10 μM more potently than phenytoin, a clinically used sodium channel blocker, a potential binding mode for (S)-hermitamide B in the BTX-binding site, and electrophysiology showing that these compounds are potent blockers of the hNav1.2 voltage-gated sodium channel.
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影响因子：
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作者：
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通讯作者：
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影响因子：
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作者：
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DOI：
10.1073/pnas.93.17.9270
发表时间：
1996-08-20
影响因子：
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作者：
Ragsdale, DS;McPhee, JC;Catterall, WA
通讯作者：
Catterall, WA