Omega conotoxins
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United States of America Patent
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Mar 18, 2014
Grant Date -
Mar 4, 2010
app pub date -
Nov 2, 2007
filing date -
Nov 4, 2006
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Abstract
The present invention relates to a method for increasing the binding reversibility of a ω-conotoxin to a N-type calcium channel, which comprises preparing a ω-conotoxin having a Ile and/or Ala residue at a position of amino acid (11 and/or 12), respectively in the second loop between cysteine residues (2 and 3) of the ω-conotoxin represented by the formula I, such that the prepared ω-conotoxin has the increased binding reversibility to N-type calcium channel. In addition, the present invention relates to a novel ω-conotoxin and a pharmaceutical composition having plausible properties in view of blocking activity to and specificity to N-type calcium channel, and dramatically improved binding reversibility to N-type calcium channel.
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