Universidad Nacional AutÓnoma De MÉxico

Lourival Domingos Possani-Postay

Rezsö Gáspár

György Panyi

Consuelo Garcia-Rodriguez

Barbara Selisko

Baltazar Becerril-Lujan

Angelina Ramirez-Navarro

Zoltán S Varga

Saida Patricia Salas-Castillo

Georgina Gurrola-Briones

César Vicente Ferreira Batista

Fernando Zamudio-Zu&ntilde;iga

Potassium channels Kv1.3 are known to be implicated in immunological diseases and graft rejections. Disclosed are peptides capable of blocking with high affinity and specificity potassium channels Kv1.3, their pharmaceutical compositions, and methods for their use to block Kv1.3 potassium channels, to treat various immunological conditions and to diagnostic applications. Methods for their chemical synthesis and correct folding are also disclosed. Exemplary peptides correspond to protein components (Vm23 and Vm24) isolated from the venom of the Mexican scorpion. Vm23 and Vm24 bind to hKv1.3 channels in an almost irreversible manner, showing a Kd value in the order of 3 picomolar range, when applied to human lymphocytes cultures in vitro. Vm24 was chemically synthesized and used in in vivo experiments to successfully treat sensitized rats (on the DTH-response). Neither Vm24 nor synthetic Vm24 is toxic to mice when injected at relatively high concentrations (assayed up to 10,000 micrograms per kilogram mouse body weight). These peptides (Vm24 and Vm23) and their functional equivalent analogs with at least 83% of sequence identity are lead compounds, candidates for the treatment of various immunological conditions and diagnostic applications.

Vm23 and Vm24, two scorpion peptides that block human T-lymphocyte potassium channels (sub-type Kv1.3) with high selectivity and decrease the in vivo DTH-responses in rats

This invention provides insecticidally effective toxins isolated from the venom of the Mexican scorpions of the genus Centruroides and the cDNA encoding one of the toxins.

Primary sequence and cDNA of insecticidally effective toxins from scorpions of the genus centruroides

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Morelos, Mexico

Lourival Domingos Possani-Postay