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

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,...

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Hauptverfasser: GURROLA-BRIONES GEORGINA, SALAS-CASTILLO SAIDA PATRICIA, FERREIRA BATISTA CESAR VICENTE, POSSANI POSTAY LOURIVAL DOMINGOS, GASPAR REZSOE, PANYI GYOERGY, VARGA ZOLTAN S
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creator GURROLA-BRIONES GEORGINA
SALAS-CASTILLO SAIDA PATRICIA
FERREIRA BATISTA CESAR VICENTE
POSSANI POSTAY LOURIVAL DOMINGOS
GASPAR REZSOE
PANYI GYOERGY
VARGA ZOLTAN S
description 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 Vaejovis mexicanus smithi. 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 microgr
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language chi ; eng
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subjects CHEMISTRY
HUMAN NECESSITIES
HYGIENE
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES
MEASURING
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PHYSICS
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
TESTING
title 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
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