Use of Kv1.3 Blockers for Inflammatory Skin Conditions

作者：Nguyen W; Howard B L; Neale D S; Thompson P E; White P J; Wulff H; M****lack D T^*

来源：Current Medicinal Chemistry, 2010, 17(26): 2882-2896.

DOI：10.2174/092986710792065072

• Psoriasis
• Kv1.3 channel
• inflammation
• drug design
• autoimmune disorder

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.

• 出版日期2010-9