Harvey Andrew J, Gable Robert W, Baell Jonathan B
The Walter and Eliza Hall, Institute of Medical Research, Biotechnology Centre, 4 Research Avenue, La Trobe R and D Park, Bundoora 3086, Australia.
Bioorg Med Chem Lett. 2005 Jul 1;15(13):3193-6. doi: 10.1016/j.bmcl.2005.05.014.
The ShK toxin is a polypeptide that blocks the Kv1.3 potassium channel in T-lymphocytes and has been identified as a potential therapeutic for multiple sclerosis. ShK is well characterised in terms of structure and binding, offering an attractive target for the design of structural and functional mimetics. Building on our previous success in developing rationally designed peptidomimetics of ShK, we report a novel mimetic of the K22-Y23-R24 residues of the peptide. The mimetic was shown to inhibit the Kv1.3 channel with moderate activity.
ShK毒素是一种多肽，可阻断T淋巴细胞中的Kv1.3钾通道，已被确定为多发性硬化症的一种潜在治疗方法。ShK在结构和结合方面已得到充分表征，为设计结构和功能模拟物提供了一个有吸引力的靶点。基于我们之前在开发合理设计的ShK肽模拟物方面的成功，我们报道了一种该肽K22 - Y23 - R24残基的新型模拟物。该模拟物显示出以中等活性抑制Kv1.3通道的作用。
