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(Received for publication, February 5, 1996, and in revised form, April 8, 1996)
From the Department of Pharmacology, University of Washington,
Seattle, Washington 98195
Volume 271, Number 27,
Issue of July 5, 1996
pp. 15950-15962
©1996 by The American Society for Biochemistry and Molecular Biology, Inc.
-Scorpion
Toxin and Sea Anemone Toxin in the S3-S4 Extracellular Loop in Domain
IV of the Na+ Channel Subunit
-Scorpion toxins and sea anemone toxins bind
to a common extracellular site on the Na+ channel and
inhibit fast inactivation. Basic amino acids of the toxins and domains
I and IV of the Na+ channel subunit have been
previously implicated in toxin binding. To identify acidic residues
required for toxin binding, extracellular acidic amino acids in domains
I and IV of the type IIa Na+ channel subunit were
converted to neutral or basic amino acids using site-directed
mutagenesis, and altered channels were transiently expressed in tsA-201
cells and tested for 125I--scorpion toxin binding.
Conversion of Glu1613 at the extracellular end of
transmembrane segment IVS3 to Arg or His blocked measurable
-scorpion toxin binding, but did not affect the level of expression
or saxitoxin binding affinity. Conversion of individual residues in the
IVS3-S4 extracellular loop to differently charged residues or to Ala
identified seven additional residues whose mutation caused significant
effects on binding of -scorpion toxin or sea anemone toxin.
Moreover, chimeric Na+ channels in which amino acid
residues at the extracellular end of segment IVS3 of the subunit of
cardiac Na+ channels were substituted into the type IIa
channel sequence had reduced affinity for -scorpion toxin
characteristic of cardiac Na+ channels.
Electrophysiological analysis showed that E1613R has 62- and 82-fold
lower affinities for -scorpion and sea anemone toxins, respectively.
Dissociation of -scorpion toxin is substantially accelerated at all
potentials compared to wild-type channels. -Scorpion toxin binding
to wild type and E1613R had similar voltage dependence, which was
slightly more positive and steeper than the voltage dependence of
steady-state inactivation. These results indicate that nonidentical
amino acids of the IVS3-S4 loop participate in -scorpion toxin and
sea anemone toxin binding to overlapping sites and that neighboring
amino acid residues in the IVS3 segment contribute to the difference in
-scorpion toxin binding affinity between cardiac and neuronal
Na+ channels. The results also support the hypothesis that
this region of the Na+ channel is important for coupling
channel activation to fast inactivation.
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