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

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.

journal_name

J Proteome Res

authors

Yin SJ,Jiang L,Yi H,Han S,Yang DW,Liu ML,Liu H,Cao ZJ,Wu YL,Li WX

doi

10.1021/pr800494a

subject

Has Abstract

pub_date

2008-11-01 00:00:00

pages

4890-7

issue

11

eissn

1535-3893

issn

1535-3907

journal_volume

7

pub_type

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