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Ivermectin and its target molecules: shared and unique modulation mechanisms of ion channels and receptors by ivermectin.
Chen, I-Shan; Kubo, Yoshihiro.
Afiliación
  • Chen IS; Division of Biophysics and Neurobiology, Department of Molecular and Cellular Physiology, National Institute for Physiological Sciences, Okazaki, 444-8585, Japan.
  • Kubo Y; Department of Physiological Sciences, School of Life Science, SOKENDAI (The Graduate University for Advanced Studies), Hayama, 240-0193, Japan.
J Physiol ; 596(10): 1833-1845, 2018 05 15.
Article en En | MEDLINE | ID: mdl-29063617
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 Omura 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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Ivermectina / Activación del Canal Iónico / Receptores Citoplasmáticos y Nucleares / Canales de Cloruro / Canales de Potasio Rectificados Internamente Asociados a la Proteína G / Receptores Purinérgicos P2X4 / Antiparasitarios Límite: Animals / Humans Idioma: En Revista: J Physiol Año: 2018 Tipo del documento: Article País de afiliación: Japón Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Ivermectina / Activación del Canal Iónico / Receptores Citoplasmáticos y Nucleares / Canales de Cloruro / Canales de Potasio Rectificados Internamente Asociados a la Proteína G / Receptores Purinérgicos P2X4 / Antiparasitarios Límite: Animals / Humans Idioma: En Revista: J Physiol Año: 2018 Tipo del documento: Article País de afiliación: Japón Pais de publicación: Reino Unido