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2. 发明授权

US07235521B1 Previns as specific inhibitors and therapeutic agents for botulinum toxin B and tetanus neurotoxins 失效
标题翻译：前列腺素作为肉毒杆菌毒素B和破伤风神经毒素的特异性抑制剂和治疗剂
公开(公告)号：US07235521B1
公开(公告)日：2007-06-26
申请号：US09979101
申请日：2000-05-15
申请人： Richard K. Gordon , Deborah R. Moorad , Bhupendra P. Doctor , Gregory E. Garcia
发明人： Richard K. Gordon , Deborah R. Moorad , Bhupendra P. Doctor , Gregory E. Garcia
IPC分类号： A61K38/00
CPC分类号： C12Q1/37 , G01N2333/95 , G01N2500/00
摘要： The compounds of the invention are generally described by the formula (1): B1Z*2B3Z*4X*5Q6F7X8X9X10X11, (2): B1X2X3X4X5Q6F7X8X9X10X11, or (3): B1X2B3X4Z5Q6F7Z8X9X10X11 and the salts, esters, amides, and acyl forms thereof. Each position represented by a letter indicates a single amino acid residue: B is a basic or polar/large amino acid or a modified form thereof; X is a small or hydrophobic amino acid or a modified form thereof; X* is a small or polar/large amino acid or a modified form thereof; Z is a polar/large or hydrophobic amino acid or a modified form thereof; Z* is Proline or a polar/large or hydrophobic amino acid or a modified form thereof. As described below, one or more of the peptide linkages between the amino acid residues may be replaced by a peptide linkage mimic. These compounds may be used as molecular building blocks to create compounds that are optimized for inhibiting the protease activity of Botulinum B and tetanus toxins.
摘要翻译：本发明的化合物通常由式（1）描述：B 1 Z * 2 B 3 Z * 4 < 5×6×6×6××××××××××××××××××××××××××××××××××××××××××< （2）：B 1 X 2 X 3 X 2 X 2 X 3 5 5 5 或（3）：B 1 X 2 B 3 3 5 X 5 5 5 它们的盐，酯，酰胺和酰基形式。由字母表示的每个位置表示单个氨基酸残基：B是碱性或极性/大氨基酸或其修饰形式; X是小或疏水性氨基酸或其修饰形式; X *是小或极/大氨基酸或其修饰形式; Z是极性/大或疏水性氨基酸或其修饰形式; Z *是脯氨酸或极性/大或疏水性氨基酸或其修饰形式。如下所述，氨基酸残基之间的一个或多个肽键可以被肽键模拟物代替。这些化合物可用作分子结构单元以产生针对抑制肉毒杆菌B和破伤风毒素的蛋白酶活性而优化的化合物。

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