Structural basis of a potent peptide inhibitor designed for Kv1.3 channel, a therapeutic target of autoimmune disease.

@article{Han2008StructuralBO,
  title={Structural basis of a potent peptide inhibitor designed for Kv1.3 channel, a therapeutic target of autoimmune disease.},
  author={Song Han and Hong Yi and Shi-Jin Yin and Zongyun Chen and Hui Liu and Zhijian Cao and Yingliang Wu and Wenxin Li},
  journal={The Journal of biological chemistry},
  year={2008},
  volume={283 27},
  pages={19058-65}
}
The potassium channel Kv1.3 is an attractive pharmacological target for immunomodulation of T cell-mediated autoimmune diseases. Potent and selective blockers of Kv1.3 are potential therapeutics for treating these diseases. Here we describe the design of a new peptide inhibitor that is potent and selective for Kv1.3. Three residues (Gly(11), Ile(28), and Asp(33)) of a scorpion toxin BmKTX were substituted by Arg(11), Thr(28), and His(33), resulting in a new peptide, named ADWX-1. The ADWX-1… CONTINUE READING