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Different relevance of inactivation and F468 residue in the mechanisms of hEag1 channel blockage by astemizole, imipramine and dofetilide

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APA

Gómez Varela, David & Contreras Jurado, Silvia Constanza & Furini, Simone & García Ferreiro, Rafael & Stühmer, Walter & Pardo, Luis A. .Different relevance of inactivation and F468 residue in the mechanisms of hEag1 channel blockage by astemizole, imipramine and dofetilide.

ISO 690

Gómez Varela, David & Contreras Jurado, Silvia Constanza & Furini, Simone & García Ferreiro, Rafael & Stühmer, Walter & Pardo, Luis A.. Different relevance of inactivation and F468 residue in the mechanisms of hEag1 channel blockage by astemizole, imipramine and dofetilide.

https://hdl.handle.net/20.500.12080/26187
dc.contributor.author Gómez Varela, David
dc.contributor.author Contreras Jurado, Silvia Constanza
dc.contributor.author Furini, Simone
dc.contributor.author García Ferreiro, Rafael
dc.contributor.author Stühmer, Walter
dc.contributor.author Pardo, Luis A.
dc.date.accessioned 2021-11-10T16:52:25Z
dc.date.available 2021-11-10T16:52:25Z
dc.date.created 2006-08-28
dc.identifier.uri https://hdl.handle.net/20.500.12080/26187
dc.description.abstract The relevance of a point mutation at the C-terminal end of the S6 helix (F468) and the introduction of C-type inacti vation in the blockage of hEag1 channels by astemizole, imipra mine and dofetilide was tested. C-type inactivation decreased block by astemizole and dofetilide but not imipramine, suggest ing different binding sites in the channel. F468C mutation in creased IC50 for astemizole and imipramine but in contrast to HERG channels, only slightly for dofetilide. Together with mea surements on recovery of blocking, our observations indicate that the mechanism of hEag1 blockage by each of these drugs is dif ferent, and suggest relevant structural differences between hEag1 and HERG channels es_ES
dc.format application/pdf es_ES
dc.language eng es_ES
dc.rights CC-BY es_ES
dc.rights.uri http://creativecommons.org/licenses/by/4.0/deed.es es_ES
dc.subject Two-electrode voltage clamp; Xenopus oocytes; Ether a` go-go; Potassium channels; Mutagenesis; Docking es_ES
dc.title Different relevance of inactivation and F468 residue in the mechanisms of hEag1 channel blockage by astemizole, imipramine and dofetilide es_ES
dc.type info:eu-repo/semantics/article es_ES
dc.rights.accessrights info:eu-repo/semantics/openAccess es_ES
dc.identifier.location N/A es_ES


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