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Use of Kv1.3 Blockers for Inflammatory Skin Conditions

机译:使用Kv1.3阻滞剂治疗炎症性皮肤病

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Recent results using animal models of inflammatory skin conditions have shown that blockers of the voltage-gated potassium channel, Kv1.3 hold great promise for clinical utility. Kv1.3 blockers act as immunosuppressants by modulating the various subsets of inflammatory T and B cells involved in autoimmune disorders. While peptidic inhibitors based on naturally occurring venoms demonstrate potent and selective Kv1.3 blockade, these require parenteral administration and may face potential immunogenicity problems. Small molecule blockers show considerable diversity, however selectivity over other Kv1-family channels has been difficult to achieve. More recent advances have added to the evidence that Kv1.3 channels are a suitable therapeutic target and that the development of novel and selective agents will herald new drugs for inflammatory skin disorders.
机译:使用炎症性皮肤病的动物模型的最新结果表明,电压门控钾通道Kv1.3的阻滞剂具有广阔的临床应用前景。 Kv1.3阻滞剂通过调节参与自身免疫性疾病的炎性T细胞和B细胞的各种亚群而充当免疫抑制剂。虽然基于天然毒液的肽类抑制剂表现出有效的和选择性的Kv1.3阻断作用,但这些药物需要肠胃外给药,可能面临潜在的免疫原性问题。小分子阻滞剂显示出相当大的多样性,但是很难实现对其他Kv1家族通道的选择性。最近的进展增加了证据,证明Kv1.3通道是合适的治疗靶标,新型选择性药物的开发将预示着用于治疗炎症性皮肤病的新药物。

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