2k4u | pdb_00002k4u

Solution structure of the SCORPION TOXIN ADWX-1

spinqualitylabelsall models 2k4u, 20 NMR models Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 2k4u is a 1 chain structure with sequence from Buthus martensi. Full experimental information is available from OCA. For a guided tour on the structure components use FirstGlance. Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function [KAX36_MESMA] Blocks voltage-gated potassium channels. At 2 uM, blocks rat Kv1.1/KCNA1 and Kv1.3/KCNA3, has a strong effect on rat Kv1.2/KCNA2 and Kv1.6/KCNA6 as well as a moderate effect on Shaker IR. Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMed 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. Different Residues in Channel Turret Determining the Selectivity of ADWX-1 Inhibitor Peptide between Kv1.1 and Kv1.3 Channels.,Yin SJ, Jiang L, Yi H, Han S, Yang DW, Liu ML, Liu H, Cao ZJ, Wu YL, Li WX J Proteome Res. 2008 Nov 7;7(11):4890-4897. Epub 2008 Oct 21. PMID:18937510 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Potassium channel toxin

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