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Channels

Sticking to nooks and crannies

Nature Chemical Biology volume 9, pages 473–474 (2013)Cite this article

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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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Figure 1: Structural models of Psora-4 binding to Kv1.5 and PAP-1 binding to Kv1.3.

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Authors and Affiliations

  1. Heike Wulff is in the Department of Pharmacology and Vladimir Yarov-Yarovoy is in the Department of Physiology & Membrane Biology, School of Medicine, University of California–Davis, Davis, California, USA.,

    Heike Wulff & Vladimir Yarov-Yarovoy

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  1. Heike Wulff
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  2. Vladimir Yarov-Yarovoy
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Correspondence to Heike Wulff or Vladimir Yarov-Yarovoy.

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Competing interests

H.W. is an inventor on a University of California patent claiming PAP-1 for immunosuppression. This patent has been licensed by Airmid, Inc., a start-up company for which H.W. is a scientific founder. Airmid has licensed on the PAP-1 patent to Circassia Ltd. (Oxford, UK) for development as a topical for psoriasis.

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Wulff, H., Yarov-Yarovoy, V. Sticking to nooks and crannies. Nat Chem Biol 9, 473–474 (2013). https://doi.org/10.1038/nchembio.1292

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