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公开(公告)号：US5840697A
公开(公告)日：1998-11-24
申请号：US660747
申请日：1996-06-06
摘要： The present invention relates to novel family of peptides which inhibit calmodulin and which have the general structure Ac-A1-B2-C3-D4-E5-F6-NH.sub.2, (SEQ ID No. 1), wherein A1 is (D)Leu or Leu, B2 is (D)Gln, Gln, (D)Trp, or Trp, C3 is (D)Arg, Arg, (D)Ile, or Ile, D4 is (D)Ile, Ile, (D)His, or His, E5 is (D)Leu, Leu, (D)His, or His, and F6 is (D)Trp, Trp, (D)Arg, or Arg. The novel peptides can be used to inhibit the activity of calmodulin. In addition, the present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a calmodulin-inhibitor peptide. These compositions can be used to treat calmodulin related disorders.
摘要翻译： 本发明涉及抑制钙调蛋白并具有通用结构Ac-A1-B2-C3-D4-E5-F6-NH2（SEQ ID No.1）的新型家族，其中A1是（D）Leu或 Leu，B2是（D）Gln，Gln，（D）Trp或Trp，C3是（D）Arg，Arg，（D）Ile或Ile，D4是（D）Ile，Ile，（D） 或His，E5为（D）Leu，Leu，（D）His或His，F6为（D）Trp，Trp，（D）Arg或Arg。 新型肽可用于抑制钙调蛋白的活性。 此外，本发明涉及包含药学上可接受的载体和钙调蛋白抑制剂肽的药物组合物。 这些组合物可用于治疗钙调蛋白相关疾病。
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公开(公告)号：US5624902A
公开(公告)日：1997-04-29
申请号：US485396
申请日：1995-06-07
摘要： The present invention relates to novel family of peptides which inhibit calmodulin and which have the general structure Ac-(D)Leu-A1-B2-C3-D4-E5-NH.sub.2, wherein A1 is (D)Gln or (D)Trp, B2 is (D)Arg or (D)Ile, C3 is (D)Ile or (D)His, D4 is (D)Leu or (D)His and E5 is (D)Trp or (D)Arg. The novel peptides can be used to inhibit the activity of calmodulin. In addition, the present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a calmodulin-inhibitor peptide. These compositions can be used to treat calmodulin related disorders.
摘要翻译： 本发明涉及抑制钙调蛋白并具有通式结构Ac-（D）Leu-A1-B2-C3-D4-E5-NH2的新型家族，其中A1为（D）Gln或（D）Trp， B2是（D）Arg或（D）Ile，C3是（D）Ile或（D）His，D4是（D）Leu或（D）His和E5是（D）Trp或（D）Arg。 新型肽可用于抑制钙调蛋白的活性。 此外，本发明涉及包含药学上可接受的载体和钙调蛋白抑制剂肽的药物组合物。 这些组合物可用于治疗钙调蛋白相关疾病。
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公开(公告)号：US5814470A
公开(公告)日：1998-09-29
申请号：US888562
申请日：1997-07-07
IPC分类号： C07K14/435 , G01N33/53
CPC分类号： C07K14/43572 , Y10S436/807 , Y10S436/815
摘要： Sets and libraries of sets of polypeptides that are related in sequence to melittin are disclosed that have antimicrobial, hemolytic and hydrolytically catalytic activities, as are processes for making and using the same. A contemplated set is a mixture of equimolar amounts of a polypeptide of SEQ ID NO:2, and more preferably SEQ ID NO:3.
摘要翻译： 公开了与蜂毒肽序列相关的多肽组和文库，其具有抗微生物，溶血和水解催化活性，以及制备和使用它们的方法。 预期的组是等摩尔量的SEQ ID NO：2的多肽，更优选SEQ ID NO：3的混合物。
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公开(公告)号：US5645996A
公开(公告)日：1997-07-08
申请号：US295086
申请日：1994-08-24
IPC分类号： C07K14/435 , G01N33/53
CPC分类号： C07K14/43572 , Y10S436/807 , Y10S436/815
摘要： Sets and libraries of sets of polypeptides that are related in sequence to melittin are disclosed that have antimicrobial, hemolytic and hydrolyrically catalytic activities, as are processes for making and using the same. A contemplated set is a mixture of equimolar amounts of a polypeptide of SEQ ID NO:2, and more preferably SEQ ID NO:3.
摘要翻译： 公开了与蜂毒肽序列相关的多肽组和文库，其具有抗微生物，溶血和水解催化活性，以及制备和使用它们的方法。 预期的组是等摩尔量的SEQ ID NO：2的多肽，更优选SEQ ID NO：3的混合物。
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公开(公告)号：US5582997A
公开(公告)日：1996-12-10
申请号：US295085
申请日：1994-08-24
IPC分类号： C07K7/08 , G01N33/68 , G01N33/53 , G01N33/531
摘要： Polypeptides, sets and libraries of sets of polypeptides that are related in sequence to the polypeptide of SEQ ID NO:1 are disclosed that have antimicrobial, hemolytic and hydrolytically catalytic activities, as are processes for making and using the same. A contemplated set is a mixture of equimolar amounts of a polypeptide of SEQ ID NO:2. Particularly preferred polypeptides include those of SEQ ID NOs:3-9.
摘要翻译： 公开了具有抗菌，溶血和水解催化活性的与SEQ ID NO：1的多肽序列相关的多肽多肽，组和多组文库，以及制备和使用它们的方法。 预期的组是等摩尔量的SEQ ID NO：2的多肽的混合物。 特别优选的多肽包括SEQ ID NO：3-9的多肽。
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公开(公告)号：US5440016A
公开(公告)日：1995-08-08
申请号：US79445
申请日：1993-06-18
CPC分类号： C07K7/06 , C07K5/0215 , C07K5/1019
摘要： Peptides having Anti-microbial activity and having the formula (KFmoc)ZZZ-NH.sub.2, wherein Z is an amino acid are disclosed. Also disclosed are peptides having anti-trypsin activity and having the formula Ac-rypwz-NH.sub.2, wherein z is a D-amino acid. Also disclosed are compositions containing these peptides and methods of using them.
摘要翻译： 公开了具有抗微生物活性并具有式（KFmoc）ZZZ-NH 2的肽，其中Z是氨基酸。 还公开了具有抗胰蛋白酶活性并具有式Ac-rypwz-NH 2的肽，其中z是D-氨基酸。 还公开了含有这些肽的组合物和使用它们的方法。
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公开(公告)号：US5698673A
公开(公告)日：1997-12-16
申请号：US434761
申请日：1995-05-04
CPC分类号： C07K7/06 , C07K5/0215 , C07K5/1019
摘要： Disclosed are peptides having anti-mellitin activity and having the formulae AC-IVILZZ-NH.sub.2, wherein Z is an amino acid. Also disclosed are compositions containing these peptides and methods of using them.
摘要翻译： 公开了具有抗梅毒素活性并具有式AC-IVILZZ-NH 2的肽，其中Z是氨基酸。 还公开了含有这些肽的组合物和使用它们的方法。
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公开(公告)号：US07022882B2
公开(公告)日：2006-04-04
申请号：US10381956
申请日：2001-10-05
IPC分类号： C07C211/13 , C07C211/27 , C07C215/52 , A61K31/135
CPC分类号： C07C215/54 , A61K31/00 , A61K31/137 , C07B2200/07 , C07C211/27 , C40B40/00
摘要： Neuroprotectant agents are provided which do not contain peptides and axe protected from the degradation that limits the use of peptide-based drugs in systemic circulation. With great selectivity for NMDA receptors, the agents exert an open channel block on NMDA receptors, and protect neuronal cells containing such receptors from excitatoxic cell death.
摘要翻译： 提供的神经保护剂不含有限制肽系药物在体循环中使用的降解的肽和斧头。 对NMDA受体具有很好的选择性，该试剂在NMDA受体上发挥开放通道阻断，并保护含有此类受体的神经元细胞免于兴奋性细胞死亡。
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9.发明授权公开(公告)号：US06359144B1
公开(公告)日：2002-03-19
申请号：US09018173
申请日：1998-02-03
申请人： John M. Ostresh , Jean-Philippe Meyer , Colette T. Dooley , Sylvie E. Blondelle , Christa C. Schoner , Richard A. Houghten
发明人： John M. Ostresh , Jean-Philippe Meyer , Colette T. Dooley , Sylvie E. Blondelle , Christa C. Schoner , Richard A. Houghten
IPC分类号： C07D40302
CPC分类号： C07D487/04 , C40B40/04
摘要： The invention provides a rapid approach for combinatorial synthesis and screening of combinatorial libraries of bicyclic guanidine compounds. The present invention further provides the compounds made by the combinatorial synthesis and individually as well as methods of using the same.
摘要翻译： 本发明提供了组合合成和筛选双环胍化合物组合文库的快速方法。 本发明还提供了通过组合合成制备的化合物及其使用方法。
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公开(公告)号：US5235038A
公开(公告)日：1993-08-10
申请号：US643343
申请日：1991-01-22
IPC分类号： A61K38/00 , C07K14/435
CPC分类号： C07K14/43572 , A61K38/00 , Y10S530/858
摘要： A compound comprising an analogue of the melittin peptide having the following structural formula: ##STR1## wherein at least one and no more than four amino acid residues are omitted from the peptide, or at least one of amino acid residues 1-6, 8-18, or 20-26 in the peptide is substituted with a hydrophobic residue, provided that no more than two of amino acid residues 21-26 is substituted with a hydrophobic residue. Such deletion and substitution analogues are useful as antibiotics, antimicrobial agents, antifungal agents, anti-tumor agents, antiviral agents, or agents which stimulate wound healing.
摘要翻译： 包含具有以下结构式的蜂毒肽的类似物的化合物：其中从肽中除去至少一个不超过四个氨基酸残基，或至少一个氨基酸（SEQ ID NO： 肽中的残基1-6,8-18或20-26被疏水残基取代，条件是不超过两个氨基酸残基21-26被疏水残基取代。 这种缺失和取代类似物可用作抗生素，抗微生物剂，抗真菌剂，抗肿瘤剂，抗病毒剂或刺激伤口愈合的药剂。
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