Article
Molecular dynamics and functional studies define a hot spot of crystal contacts essential for PcTx1 inhibition of acid-sensing ion channel 1a.
British journal of pharmacology - 1 Oct 2015
Saez Natalie J, Deplazes Evelyne, Cristofori-Armstrong Ben, Chassagnon Irène R, Lin Xiaozhen, Mobli Mehdi, Mark Alan E, Rash Lachlan D, King Glenn F
Abstract excerpt
BACKGROUND AND PURPOSE: The spider-venom peptide PcTx1 is the most potent and selective inhibitor of acid-sensing ion channel (ASIC) 1a. It has centrally acting analgesic activity and is neuroprotective in rodent models of ischaemic stroke. Understanding the molecular details of the PcTx1 : ASIC1a interaction should facilitate development of therapeutically useful ASIC1a modulators. Previously, we showed that...
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