Ivermectin and its target molecules: shared and unique modulation mechanisms of ion channels and receptors by ivermectin
Year: 2017
Type: review
Abstract: Ivermectin (IVM) is an antiparasitic drug that is used worldwide and rescues hundreds of millions of people from onchocerciasis and lymphatic filariasis. It was discovered by Satoshi Ōmura and William C. Campbell, to whom the 2015 Nobel Prize in Physiology or Medicine was awarded. It kills parasites by activating glutamate‐gated Cl− channels, and it also targets several ligand‐gated ion channels and receptors, including Cys‐loop receptors, P2X4 receptors and fernesoid X receptors. Recently, we found that IVM also activates a novel target, the G‐protein‐gated inwardly rectifying K+ channel, and also identified the structural determinant for the activation. In this review, we aim to provide an update and summary of recent progress in the identification of IVM targets, as well as their modulation mechanisms, through molecular structures, chimeras and site‐directed mutagenesis, and molecular docking and modelling studies. image
Source: The Journal of Physiology
DOI: 10.1113/jp275236
Authors: I‐Shan Chen, Yoshihiro Kubo
Language: English
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: green
Awards: Analyses of an orphan metabotropic receptor which plays a role in the long term retention of memory, and a secretory protein encoded by its splice variant, The physiological ligand and activation mechanisms of an orphan metabotropic receptor Prrt3, Analysis of dynamic structural rearrangements of functioning ion channels by fluorescent unnatural amino acid
OpenAlex ID: W2765521280