Peptide sr11a from Conus spurius is a novel peptide blocker for Kv1 potassium channels
Por:
Aguilar M.B., Pérez-Reyes L.I., López Z., de la Cotera, EPH, Falcón A., Ayala C., Galván M., Salvador C., Escobar L.I.
Publicada:
1 jul 2010
Resumen:
More than a hundred conotoxins are known today and from them, only seven conopeptides have been identified to target voltage-gated potassium channels (Kv). Conotoxin sr11a belongs to the I(2)-superfamily which is characterized by four disulfide bridges and provokes muscle stiffness when injected intracranially in mice. The aim of this work was to test the biological activity of sr11a on recombinant voltage-gated Kv1 potassium channels expressed in Xenopus laevis oocytes. Peptide sr11a was purified by high-performance liquid chromatography from the venom of the vermivorous Conus spurius. We found that peptide sr11a inhibits the delayed rectifiers Kv1.2 and Kv1.6 but had not effect on the slowly inactivating Kv1.3 channel. The functional dyad composed of a basic Lys and a hydrophobic amino acid residue is a crucial structural element, regarding the binding properties and blocking activities of more than a hundred K(+) channel toxins. Peptide sr11a does not contain Lys residues and then,
Filiaciones:
Aguilar M.B.:
Univ Nacl Autonoma Mexico, Lab Neurofarmacol, Dept Neurobiol Celular & Mol, Inst Neurobiol, Queretaro 76230, Mexico
Pérez-Reyes L.I.:
Univ Nacl Autonoma Mexico, Fac Med, Dept Fisiol, Mexico City 70250, DF, Mexico
López Z.:
Univ Nacl Autonoma Mexico, Fac Med, Dept Fisiol, Mexico City 70250, DF, Mexico
de la Cotera, EPH:
Univ Nacl Autonoma Mexico, Lab Neurofarmacol, Dept Neurobiol Celular & Mol, Inst Neurobiol, Queretaro 76230, Mexico
Falcón A.:
Univ Nacl Autonoma Mexico, Lab Neurofarmacol, Dept Neurobiol Celular & Mol, Inst Neurobiol, Queretaro 76230, Mexico
Ayala C.:
Departamento de Química, Universidad Autónoma Metropolitana-Iztapalapa, San Rafael Atlixco 186, Iztapalapa, México, DF 09340, Mexico
Galván M.:
Departamento de Química, Universidad Autónoma Metropolitana-Iztapalapa, San Rafael Atlixco 186, Iztapalapa, México, DF 09340, Mexico
Salvador C.:
Univ Nacl Autonoma Mexico, Fac Med, Dept Fisiol, Mexico City 70250, DF, Mexico
Escobar L.I.:
Univ Nacl Autonoma Mexico, Fac Med, Dept Fisiol, Mexico City 70250, DF, Mexico
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