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Different residues in channel turret determining the selectivity of ADWX-1 inhibitor peptide between Kv1.1 and Kv1.3 channels.

Shi-Jin Yin, Ling Jiang, Hong Yi, Song Han, Dai-Wen Yang, Mai-Li Liu, Hui Liu, Zhi-Jian Cao, Ying-Liang Wu, Wen-Xin Li

J. Proteome Res., 2008 Nov , 7, 4890-7

The low selectivity of Kv1 peptide inhibitors for specific isoforms makes them poor candidates for the development of theraputics. Using combined approaches, we showed that the Kv1 turret is the critical determinant for ADWX-1 peptide inhibitor selectivity of Kv1.3 over Kv1.1. Mutation of Kv1.1 turret residues to match the sequence of Kv1.3 lead to increased inhibition of Kv1.1 activity. These studies may lead to improvements in peptide inhibitor drug development.