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    • 8. 发明授权
    • Contryphan peptides
    • 对角han肽
    • US6153738A
    • 2000-11-28
    • US466138
    • 1999-12-21
    • Richard JacobsenElsie JimenezLourdes J. CruzBaldomero M. OliveraWilliam R. GrayMichelle GrilleyMaren WatkinsDavid R. Hillyard
    • Richard JacobsenElsie JimenezLourdes J. CruzBaldomero M. OliveraWilliam R. GrayMichelle GrilleyMaren WatkinsDavid R. Hillyard
    • A61K38/00C07K7/06C07H21/04
    • C07K7/06A61K38/00Y10S530/857
    • The present invention is directed to contryphan peptides having 6-12 amino acids, preferably including one or more D-tryptophan or D-leucine residues. The peptides of the present invention are generically termed "contryphans," although the D-leucine containing contryphans are sometimes referred to as leu-contryphans. More specifically, the present invention is directed to contryphan peptides having the general formula Xaa.sub.1 -Cys-Xaa.sub.2 -Xaa.sub.3 -Xaa.sub.4 -Pro-Xaa.sub.5 -Cys (SEQ ID NO:1), wherein Xaa.sub.1 is any amino acid or des-Xaa.sub.1, Xaa.sub.2 is Pro, 4-trans-hydroxyproline or Val, Xaa.sub.3 is D-Trp, L-Trp, D-Leu or L-Leu, preferably D-Trp or D-Leu, Xaa.sub.4 is any amino acid and Xaa.sub.5 is Trp or Tyr. When the peptide contains Xaa.sub.1, it is preferably Gly, Glu, or Lys, most preferably Gly. When Xaa.sub.3 is D- or L-Trp, Xaa.sub.2 is preferably Pro or 4-trans-hydroxyproline. When Xaa.sub.3 is D- or L-Leu, Xaa.sub.2 is preferably Val. The carboxy terminus may contain a carboxyl or an amide, preferably an amide. The present invention is further directed to the specific contryphan peptides and propeptides as described herein. The present invention is also directed to nucleic acids encoding the contryphan peptides and their propeptides as described herein. The contryphans of the present invention are useful as anticonvulsant or neuroprotective agents.
    • 本发明涉及具有6-12个氨基酸的优选肽,优选包括一个或多个D-色氨酸或D-亮氨酸残基。 本发明的肽通常被称为“contryphans”,尽管含有D-亮氨酸的对应物有时被称为leu-contryphans。 更具体地说,本发明涉及具有通式Xaa1-Cys-Xaa2-Xaa3-Xaa4-Pro-Xaa5-Cys(SEQ ID NO:1)的反式肽,其中Xaa1是任何氨基酸或des-Xaa1,Xaa2 是Pro,4-反式 - 羟基脯氨酸或Val,Xaa3是D-Trp,L-Trp,D-Leu或L-Leu,优选D-Trp或D-Leu,Xaa4是任何氨基酸,Xaa5是Trp或Tyr。 当肽含有Xaa1时,其优选为Gly,Glu或Lys,最优选为Gly。 当Xaa3为D-或L-Trp时,Xaa2优选为Pro或4-反式 - 羟脯氨酸。 当Xaa3为D-或L-Leu时,Xaa2优选为Val。 羧基末端可以含有羧基或酰胺,优选酰胺。 本发明进一步针对如本文所述的特异性抗原肽和前肽。 本发明还涉及编码本文所述的敌百虫肽及其前肽的核酸。 本发明的对策可用作抗惊厥药或神经保护剂。
    • 9. 发明授权
    • Contryphan peptides
    • 对角han肽
    • US6077934A
    • 2000-06-20
    • US61026
    • 1998-04-16
    • Richard JacobsenElsie JimenezLourdes J. CruzBaldomero M. OliveraWilliam R. GrayMichelle GrilleyMaren WatkinsDavid R. Hillyard
    • Richard JacobsenElsie JimenezLourdes J. CruzBaldomero M. OliveraWilliam R. GrayMichelle GrilleyMaren WatkinsDavid R. Hillyard
    • A61K38/00C07K7/06C07K5/00
    • C07K7/06A61K38/00Y10S530/857
    • The present invention is directed to contryphan peptides having 6-12 amino acids, preferably including one or more D-tryptophan or D-leucine residues. The peptides of the present invention are generically termed "contryphans," although the D-leucine containing contryphans are sometimes referred to as leu-contryphans. More specifically, the present invention is directed to contryphan peptides having the general formula Xaa.sub.1 -Cys-Xaa.sub.2 -Xaa.sub.3 -Xaa.sub.4 -Pro-Xaa.sub.5 -Cys (SEQ ID NO:1), wherein Xaa.sub.1, is any amino acid or des-Xaa.sub.1, Xaa.sub.2 is Pro, 4-trans-hydroxyproline or Val, Xaa.sub.3 is D-Trp, L-Trp, D-Leu or L-Leu, preferably D-Trp or D-Leu, Xaa.sub.4 is any amino acid and Xaa.sub.5 is Trp or Tyr. When the peptide contains Xaa.sub.1, it is preferably Gly, Glu, or Lys, most preferably Gly. When Xaa.sub.3 is D- or L-Trp, Xaa.sub.2 is preferably Pro or 4-trans-hydroxyproline. When Xaa.sub.3 is D- or L-Leu, Xaa.sub.2 is preferably Val. The carboxy terminus may contain a carboxyl or an amide, preferably an amide. The present invention is further directed to the specific contryphan peptides and propeptides as described herein. The present invention is also directed to nucleic acids encoding the contryphan peptides and their propeptides as described herein. The contryphans of the present invention are useful as anticonvulsant or neuroprotective agents.
    • 本发明涉及具有6-12个氨基酸的优选肽,优选包括一个或多个D-色氨酸或D-亮氨酸残基。 本发明的肽通常被称为“contryphans”,尽管含有D-亮氨酸的对应物有时被称为leu-contryphans。 更具体地,本发明涉及具有通式Xaa1-Cys-Xaa2-Xaa3-Xaa4-Pro-Xaa5-Cys(SEQ ID NO:1)的反式肽,其中Xaa1是任何氨基酸或des-Xaa1, Xaa2是Pro,4-反 - 羟脯氨酸或Val,Xaa3是D-Trp,L-Trp,D-Leu或L-Leu,优选D-Trp或D-Leu,Xaa4是任何氨基酸,Xaa5是Trp或Tyr 。 当肽含有Xaa1时,其优选为Gly,Glu或Lys,最优选为Gly。 当Xaa3为D-或L-Trp时,Xaa2优选为Pro或4-反式 - 羟脯氨酸。 当Xaa3为D-或L-Leu时,Xaa2优选为Val。 羧基末端可以含有羧基或酰胺,优选酰胺。 本发明进一步针对如本文所述的特异性抗原肽和前肽。 本发明还涉及编码本文所述的敌百虫肽及其前肽的核酸。 本发明的对策可用作抗惊厥药或神经保护剂。