ANALOGS OF SHK TOXIN AND THEIR USES IN SELECTIVE INHIBITION OF KV1.3 POTASSIUM CHANNELS
    1.
    发明公开
    ANALOGS OF SHK TOXIN AND THEIR USES IN SELECTIVE INHIBITION OF KV1.3 POTASSIUM CHANNELS 审中-公开
    新鸿基毒素的Kv1.3钾离子通道类似物及其作为选择性抑制剂

    公开(公告)号:EP1796709A2

    公开(公告)日:2007-06-20

    申请号:EP05810512.3

    申请日:2005-10-07

    IPC分类号: A61K38/00

    摘要: Analogs of ShK toxin and methods for using such ShK analogs. The ShK analogs generally 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 comprise an amino acid residue. The ShK analogs may be administered to human or non-human animal subjects to cause inhibition of potassium channels or to otherwise treat diseases or disorders. In some embodiments, the chemical entity to which the ShK toxin is attached may be chosen to provide selective inhibition of certain potassium channels (e.g., Kv1.3 channels) over other potassium channels (e.g., Kv1.1 channels). In come embodiments, the chemical entity to which the ShK toxin is attached may include a fluorophore, thereby providing a fluorophore tagged ShK analog. Such fluorophore tagged ShK analogs may be used in flow cytometry alone, or in conjunction with class II tetramers that can detect autoreactive cells.

    ANALOGS OF SHK TOXIN AND THEIR USES IN SELECTIVE INHIBITION OF KV1.3 POTASSIUM CHANNELS
    2.
    发明公开
    ANALOGS OF SHK TOXIN AND THEIR USES IN SELECTIVE INHIBITION OF KV1.3 POTASSIUM CHANNELS 审中-公开
    ANALOGA VON SHK-TOXIN UND IHRE VERWENDUNG ALS SELEKTIVE INHIBITOREN VON KV1.3-KALIUMKANÄLEN

    公开(公告)号:EP3090753A1

    公开(公告)日:2016-11-09

    申请号:EP16157419.9

    申请日:2005-10-07

    IPC分类号: A61K38/00

    摘要: Analogs of ShK toxin and methods for using such ShK analogs. The ShK analogs generally 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 comprise an amino acid residue. The ShK analogs may be administered to human or non-human animal subjects to cause inhibition of potassium channels or to otherwise treat diseases or disorders. In some embodiments, the chemical entity to which the ShK toxin is attached may be chosen to provide selective inhibition of certain potassium channels (e.g., Kv1.3 channels) over other potassium channels (e.g., Kv1.1 channels). In come embodiments, the chemical entity to which the ShK toxin is attached may include a fluorophore, thereby providing a fluorophore tagged ShK analog. Such fluorophore tagged ShK analogs may be used in flow cytometry alone, or in conjunction with class II tetramers that can detect autoreactive cells.

    摘要翻译: ShK毒素的类似物和使用这种ShK类似物的方法。 ShK类似物通常包含与具有阴离子电荷的化学实体(例如原子,分子,基团,残基,化合物,部分等)连接的ShK毒素。 在一些实施方案中,连接至ShK毒素的化学实体可以包含氨基酸残基。 可以向人类或非人类动物受试者施用ShK类似物以引起钾通道的抑制或以其它方式治疗疾病或病症。 在一些实施方案中,可以选择与其连接的ShK毒素的化学实体以提供对其它钾通道(例如,Kv1.1通道)的某些钾通道(例如,Kv1.3通道)的选择性抑制。 在实施方案中,ShK毒素所连接的化学实体可以包括荧光团,从而提供荧光标记的ShK类似物。 这种荧光标记的ShK类似物可以单独用于流式细胞术,或与可检测自身反应性细胞的II类四聚体结合使用。