Abstract
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.
Keywords: Psoriasis, Kv1.3 channel, inflammation, drug design, autoimmune disorder
Current Medicinal Chemistry
Title: Use of Kv1.3 Blockers for Inflammatory Skin Conditions
Volume: 17 Issue: 26
Author(s): W. Nguyen, B.L. Howard, D.S. Neale, P.E. Thompson, P.J. White, H. Wulff and D.T. Manallack
Affiliation:
Keywords: Psoriasis, Kv1.3 channel, inflammation, drug design, autoimmune disorder
Abstract: 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.
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Cite this article as:
Nguyen W., Howard B.L., Neale D.S., Thompson P.E., White P.J., Wulff H. and Manallack D.T., Use of Kv1.3 Blockers for Inflammatory Skin Conditions, Current Medicinal Chemistry 2010; 17 (26) . https://dx.doi.org/10.2174/092986710792065072
DOI https://dx.doi.org/10.2174/092986710792065072 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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