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ANALOGS OF SHK TOXIN AND THEIR USES IN SELECTIVE INHIBITION OF KV1.3 POTASSIUM CHANNELS

机译:SHK毒素的类似物及其在KV1.3钾离子通道选择性抑制中的应用。

摘要

Analogs of ShK toxin and methods for using such ShK analogs. The ShK analogsgenerally comprise ShK toxin attached to a chemical entity (e.g. an atom,molecule, group, residue, compound, moiety, etc.) that has an anionic charge.In some embodiments the chemical entity attached to the ShK toxin may comprisean amino acid residue. The ShK analogs may be administered to human or non-human animal subjects to cause inhibition of potassium channels or tootherwise treat diseases or disorders. In some embodiments, the chemicalentity to which the ShK toxin is attached may be chosen to provide selectiveinhibition of certain potassium channels (e.g., Kv1.3 channels) over otherpotassium channels (e.g., Kv1.1 channels). In come embodiments, the chemicalentity to which the ShK toxin is attached may include a fluorophore, therebyproviding a fluorophore tagged ShK analog. Such fluorophore tagged ShK analogsmay be used in flow cytometry alone, or in conjunction with class II tetramersthat can detect autoreactive cells.
机译:ShK毒素的类似物和使用这种ShK类似物的方法。 ShK类似物通常包含与化学实体(例如原子,带有阴离子电荷的分子,基团,残基,化合物,部分等)。在一些实施方案中,与ShK毒素连接的化学实体可以包括氨基酸残基。 ShK类似物可施用于人类或非人类人类动物个体引起钾通道抑制或否则治疗疾病或失调。在一些实施方案中,化学可以选择与ShK毒素结合的实体,以提供选择性抑制某些钾离子通道(例如Kv1.3通道)钾离子通道(例如Kv1.1通道)。在一些实施方案中,化学ShK毒素所附着的实体可以包括荧光团,从而提供荧光团标记的ShK类似物。此类荧光团标记的ShK类似物可单独用于流式细胞术,或与II类四聚体结合使用可以检测自身反应性细胞。

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