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Inhibition of Kir4.1 potassium channels by quinacrine.
Marmolejo-Murillo, Leticia G; Aréchiga-Figueroa, Iván A; Cui, Meng; Moreno-Galindo, Eloy G; Navarro-Polanco, Ricardo A; Sánchez-Chapula, José A; Ferrer, Tania; Rodríguez-Menchaca, Aldo A.
Afiliação
  • Marmolejo-Murillo LG; Centro Universitario de Investigaciones Biomédicas, Universidad de Colima, Colima, Col 28045, Mexico.
  • Aréchiga-Figueroa IA; CONACYT, Facultad de Medicina, Universidad Autónoma de San Luis Potosí, San Luis Potosí, SLP 78210, Mexico.
  • Cui M; Department of Physiology and Biophysics, Virginia Commonwealth University, School of Medicine, Richmond, VA 23298, USA.
  • Moreno-Galindo EG; Centro Universitario de Investigaciones Biomédicas, Universidad de Colima, Colima, Col 28045, Mexico.
  • Navarro-Polanco RA; Centro Universitario de Investigaciones Biomédicas, Universidad de Colima, Colima, Col 28045, Mexico.
  • Sánchez-Chapula JA; Centro Universitario de Investigaciones Biomédicas, Universidad de Colima, Colima, Col 28045, Mexico.
  • Ferrer T; Centro Universitario de Investigaciones Biomédicas, Universidad de Colima, Colima, Col 28045, Mexico. Electronic address: tania@ucol.mx.
  • Rodríguez-Menchaca AA; Departamento de Fisiología y Biofísica, Facultad de Medicina, Universidad Autónoma de San Luis Potosí, SLP 78210, Mexico. Electronic address: aldo.rodriguez@uaslp.mx.
Brain Res ; 1663: 87-94, 2017 05 15.
Article em En | MEDLINE | ID: mdl-28288868
Inwardly rectifying potassium (Kir) channels are expressed in many cell types and contribute to a wide range of physiological processes. Particularly, Kir4.1 channels are involved in the astroglial spatial potassium buffering. In this work, we examined the effects of the cationic amphiphilic drug quinacrine on Kir4.1 channels heterologously expressed in HEK293 cells, employing the patch clamp technique. Quinacrine inhibited the currents of Kir4.1 channels in a concentration and voltage dependent manner. In inside-out patches, quinacrine inhibited Kir4.1 channels with an IC50 value of 1.8±0.3µM and with extremely slow blocking and unblocking kinetics. Molecular modeling combined with mutagenesis studies suggested that quinacrine blocks Kir4.1 by plugging the central cavity of the channels, stabilized by the residues E158 and T128. Overall, this study shows that quinacrine blocks Kir4.1 channels, which would be expected to impact the potassium transport in several tissues.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Quinacrina / Canais de Potássio Corretores do Fluxo de Internalização Limite: Animals / Humans Idioma: En Revista: Brain Res Ano de publicação: 2017 Tipo de documento: Article País de afiliação: México País de publicação: Holanda
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Quinacrina / Canais de Potássio Corretores do Fluxo de Internalização Limite: Animals / Humans Idioma: En Revista: Brain Res Ano de publicação: 2017 Tipo de documento: Article País de afiliação: México País de publicação: Holanda