Literature DB >> 23868316

Channels: Sticking to nooks and crannies.

Heike Wulff, Vladimir Yarov-Yarovoy.   

Abstract

Drug design for voltage-gated ion channels has long been hampered by the absence of crystal structures and the challenge of achieving subtype selectivity. A combination of mutagenesis, electrophysiology and molecular modeling has led to the identification of a new side pocket binding site for the small molecule Psora-4 between the pore and the voltage-sensor domain of Kv1.5, offering opportunities to design allosteric ion channel modulators.

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Year:  2013        PMID: 23868316     DOI: 10.1038/nchembio.1292

Source DB:  PubMed          Journal:  Nat Chem Biol        ISSN: 1552-4450            Impact factor:   15.040


  7 in total

1.  Potassium channel block by a tripartite complex of two cationophilic ligands and a potassium ion.

Authors:  Pavel I Zimin; Bojan Garic; Silke B Bodendiek; Cédrick Mahieux; Heike Wulff; Boris S Zhorov
Journal:  Mol Pharmacol       Date:  2010-07-02       Impact factor: 4.436

2.  Design of PAP-1, a selective small molecule Kv1.3 blocker, for the suppression of effector memory T cells in autoimmune diseases.

Authors:  Alexander Schmitz; Ananthakrishnan Sankaranarayanan; Philippe Azam; Kristina Schmidt-Lassen; Daniel Homerick; Wolfram Hänsel; Heike Wulff
Journal:  Mol Pharmacol       Date:  2005-08-11       Impact factor: 4.436

3.  Atomic structure of a voltage-dependent K+ channel in a lipid membrane-like environment.

Authors:  Stephen B Long; Xiao Tao; Ernest B Campbell; Roderick MacKinnon
Journal:  Nature       Date:  2007-11-15       Impact factor: 49.962

4.  Kv1.3-blocking 5-phenylalkoxypsoralens: a new class of immunomodulators.

Authors:  Julia Vennekamp; Heike Wulff; Christine Beeton; Peter A Calabresi; Stephan Grissmer; Wolfram Hänsel; K George Chandy
Journal:  Mol Pharmacol       Date:  2004-06       Impact factor: 4.436

5.  The crystal structure of a voltage-gated sodium channel.

Authors:  Jian Payandeh; Todd Scheuer; Ning Zheng; William A Catterall
Journal:  Nature       Date:  2011-07-10       Impact factor: 49.962

6.  Side pockets provide the basis for a new mechanism of Kv channel-specific inhibition.

Authors:  Stefanie Marzian; Phillip J Stansfeld; Markus Rapedius; Susanne Rinné; Ehsan Nematian-Ardestani; Jennifer L Abbruzzese; Klaus Steinmeyer; Mark S P Sansom; Michael C Sanguinetti; Thomas Baukrowitz; Niels Decher
Journal:  Nat Chem Biol       Date:  2013-06-02       Impact factor: 16.174

7.  IUPHAR-DB: the IUPHAR database of G protein-coupled receptors and ion channels.

Authors:  Anthony J Harmar; Rebecca A Hills; Edward M Rosser; Martin Jones; O Peter Buneman; Donald R Dunbar; Stuart D Greenhill; Valerie A Hale; Joanna L Sharman; Tom I Bonner; William A Catterall; Anthony P Davenport; Philippe Delagrange; Colin T Dollery; Steven M Foord; George A Gutman; Vincent Laudet; Richard R Neubig; Eliot H Ohlstein; Richard W Olsen; John Peters; Jean-Philippe Pin; Robert R Ruffolo; David B Searls; Mathew W Wright; Michael Spedding
Journal:  Nucleic Acids Res       Date:  2008-10-23       Impact factor: 16.971

  7 in total
  3 in total

Review 1.  Discovery of KV 1.3 ion channel inhibitors: Medicinal chemistry approaches and challenges.

Authors:  Špela Gubič; Louise A Hendrickx; Žan Toplak; Maša Sterle; Steve Peigneur; Tihomir Tomašič; Luis A Pardo; Jan Tytgat; Anamarija Zega; Lucija P Mašič
Journal:  Med Res Rev       Date:  2021-05-01       Impact factor: 12.944

2.  Distinct and complementary roles for α and β isoenzymes of PKC in mediating vasoconstrictor responses to acutely elevated glucose.

Authors:  Robert Jackson; Sean Brennan; Peter Fielding; Mark W Sims; R A John Challiss; David Adlam; Iain B Squire; Richard D Rainbow
Journal:  Br J Pharmacol       Date:  2016-02-08       Impact factor: 8.739

3.  New potential binding determinant for hERG channel inhibitors.

Authors:  P Saxena; E-M Zangerl-Plessl; T Linder; A Windisch; A Hohaus; E Timin; S Hering; A Stary-Weinzinger
Journal:  Sci Rep       Date:  2016-04-12       Impact factor: 4.996

  3 in total

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