公开(公告)号：US08673856B2

公开(公告)日：2014-03-18

申请号：US12513182

申请日：2007-11-02

申请人： Jae II Kim ,  Hye Whon Rhim ,  Hyun Jeong Kim ,  Hong Won Suh ,  Soung Hun Roh ,  Jung A Yun ,  Seung Kyu Lee ,  Young Jae Eu ,  Heung Sik Na

发明人： Jae II Kim ,  Hye Whon Rhim ,  Hyun Jeong Kim ,  Hong Won Suh ,  Soung Hun Roh ,  Jung A Yun ,  Seung Kyu Lee ,  Young Jae Eu ,  Heung Sik Na

IPC分类号： A61K38/16 ,  A61K38/00 ,  C07K14/00

CPC分类号： C07K14/43504 ,  A61K38/00

摘要： 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.

摘要翻译： 本发明涉及一种增加ω-芋螺毒素与N型钙通道的结合可逆性的方法，其包括在氨基酸（11和/或其氨基酸）的位置制备具有Ile和/或Ala残基的ω-芋螺毒素， 或12）分别在由式I表示的ω-芋螺毒素的半胱氨酸残基（2和3）之间的第二环中，使得所制备的ω-芋螺毒素具有增加的对N-型钙通道的结合可逆性。 此外，本发明涉及一种新型的ω-芋螺毒素和具有似乎合理的性质的药物组合物，其特征在于阻断N-型钙通道的活性和特异性，并显着提高了对N-型钙通道的结合可逆性。