2K4U

Solution structure of the SCORPION TOXIN ADWX-1

2K4U の概要

• エントリーDOI: 10.2210/pdb2k4u/pdb
• 分子名称: Potassium channel toxin alpha-KTx 3.6 (1 entity in total)
• 機能のキーワード: kv1.1 channel, kv1.3 channel, channel turret, adwx-1 peptide selectivity, structural basis, amidation, ionic channel inhibitor, neurotoxin, potassium channel inhibitor, secreted, toxin
• 由来する生物種: Mesobuthus martensii (Chinese scorpion)
• 細胞内の位置: Secreted: Q9NII7
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 4088.98

構造登録者

Yin, S.J.,Jiang, L.,Yi, H.,Han, S.,Yang, D.W.,Liu, M.L.,Liu, H.,Cao, Z.J.,Wu, Y.L.,Li, W.X. (登録日: 2008-06-18, 公開日: 2008-12-09, 最終更新日: 2024-11-13)

主引用文献

Yin, S.J.,Jiang, L.,Yi, H.,Han, S.,Yang, D.W.,Liu, M.L.,Liu, H.,Cao, Z.J.,Wu, Y.L.,Li, W.X.
Different Residues in Channel Turret Determining the Selectivity of ADWX-1 Inhibitor Peptide between Kv1.1 and Kv1.3 Channels
J.Proteome Res., 7:4890-4897, 2008

PubMed Abstract: 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.

PubMed: 18937510
DOI: 10.1021/pr800494a

実験手法

SOLUTION NMR