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公开(公告)号:US6077934A
公开(公告)日:2000-06-20
申请号:US61026
申请日:1998-04-16
申请人: Richard Jacobsen , Elsie Jimenez , Lourdes J. Cruz , Baldomero M. Olivera , William R. Gray , Michelle Grilley , Maren Watkins , David R. Hillyard
发明人: Richard Jacobsen , Elsie Jimenez , Lourdes J. Cruz , Baldomero M. Olivera , William R. Gray , Michelle Grilley , Maren Watkins , David R. Hillyard
CPC分类号: C07K7/06 , A61K38/00 , Y10S530/857
摘要: 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.
摘要翻译: 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。
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公开(公告)号:US6153738A
公开(公告)日:2000-11-28
申请号:US466138
申请日:1999-12-21
申请人: Richard Jacobsen , Elsie Jimenez , Lourdes J. Cruz , Baldomero M. Olivera , William R. Gray , Michelle Grilley , Maren Watkins , David R. Hillyard
发明人: Richard Jacobsen , Elsie Jimenez , Lourdes J. Cruz , Baldomero M. Olivera , William R. Gray , Michelle Grilley , Maren Watkins , David R. Hillyard
CPC分类号: C07K7/06 , A61K38/00 , Y10S530/857
摘要: 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.
摘要翻译: 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。
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公开(公告)号:US5672682A
公开(公告)日:1997-09-30
申请号:US619936
申请日:1996-03-18
IPC分类号: A61K38/00 , C07K14/435 , C07K14/00
CPC分类号: C07K14/43504 , A61K38/00
摘要: A new peptide, .kappa.-conotoxin PVIIA, is disclosed. This peptide is found naturally in the cone snail Conus purpurascens and has the amino acid sequence Cys-Arg-Ile-Xaa-Asn-Gln-Lys-Cys-Phe-Gln-His-Leu-Asp-Asp-Cys-Cys-Ser-Arg-Lys-Cys-Asn-Arg-Phe-Asn-Lys-Cys-Val (SEQ ID NO:1) where Xaa represents 4-trans-hydroxyproline hydroxyproline or proline. This peptide together with a previously disclosed peptide, .delta.-conotoxin PVIA, act synergistically to rapidly immobilize fish which are injected with the two peptides. Injection of .kappa.-conotoxin PVIIA alone results in different symptoms with an injected fish becoming hyperactive and then contracting and suddenly extending all major fins. This "fin-popping" occurs repeatedly resulting in a series of jerky movements, but injection of only .kappa.-conotoxin PVIIA does not immobilize or kill the fish.
摘要翻译: 公开了一种新的肽,κ-毒素PVIIA。 这种肽天然存在于锥螺旋锥体中,具有氨基酸序列Cys-Arg-Ile-Xaa-Asn-Gln-Lys-Cys-Phe-Gln-His-Leu-Asp-Asp-Cys-Cys-Ser -Arg-Lys-Cys-Asn-Arg-Phe-Asn-Lys-Cys-Val(SEQ ID NO:1),其中Xaa表示4-反式 - 羟脯氨酸羟脯氨酸或脯氨酸。 该肽与先前公开的肽δ-毒素PVIA一起协同作用以快速固定注射了两种肽的鱼。 单独注射κ-毒素PVIIA导致不同的症状,注射的鱼变得活跃,然后收缩并突然延伸所有主要鳍。 这种“昙花一现”反复发生,导致一连串的剧烈运动,但只注射κ-毒素PVIIA不会使鱼类不能固定或杀死。
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公开(公告)号:US09669044B2
公开(公告)日:2017-06-06
申请号:US14281659
申请日:2014-05-19
IPC分类号: A61K31/7036 , A61K31/496 , A61K31/4196 , A61K31/506 , A61K31/415 , A61K31/365 , A01N43/16
CPC分类号: A61K31/7036 , A01N43/16 , A61K31/365 , A61K31/415 , A61K31/4196 , A61K31/496 , A61K31/506 , A61K2300/00 , A01N43/653 , A01N47/24
摘要: The present invention relates to novel fungicidal compound including an aminoglycoside analog having certain substituents at the 6 position of ring III that exhibit improved antifungal activity but possess minimal antibacterial properties in combination with fungicidal azoles. The aminoglycoside compounds are analogues of kanamycin A. Also provided are methods of synthesizing and methods of using the compounds of the present invention. The compounds of the present invention are useful in treating or preventing fungal disease.
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公开(公告)号:US20060014673A1
公开(公告)日:2006-01-19
申请号:US11174996
申请日:2005-07-06
申请人: Richard Layer , Karen Pemberton , Robert Jones , James Garrett , Baldomero Olivera , J. McIntosh , David Hillyard , Michelle Grilley , Maren Watkins , Ameurfina Santos , Glenn Zafaralla , A. Craig
发明人: Richard Layer , Karen Pemberton , Robert Jones , James Garrett , Baldomero Olivera , J. McIntosh , David Hillyard , Michelle Grilley , Maren Watkins , Ameurfina Santos , Glenn Zafaralla , A. Craig
IPC分类号: A61K38/16 , C07K14/435
CPC分类号: A61K38/17 , C07K14/43504
摘要: The present invention is directed to kappaA (κA) conopeptides and the use of these peptides for blocking the flow of potassium ions through voltage-gated potassium channels. The κA conopeptides include unglycosylated and O-glycosylated peptides.
摘要翻译: 本发明涉及kappaA(kappaA)肽以及这些肽用于阻断通过电压门控钾通道的钾离子流动的用途。 κA肽包括非糖基化和O-糖基化肽。
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公开(公告)号:US20140256665A1
公开(公告)日:2014-09-11
申请号:US14281659
申请日:2014-05-19
IPC分类号: A61K31/7036 , A61K31/4174 , A61K31/506 , A61K31/415 , A61K31/496 , A61K31/4196
CPC分类号: A61K31/7036 , A01N43/16 , A61K31/365 , A61K31/415 , A61K31/4196 , A61K31/496 , A61K31/506 , A61K2300/00 , A01N43/653 , A01N47/24
摘要: The present invention relates to novel fungicidal compound including an aminoglycoside analog having certain substituents at the 6 position of ring III that exhibit improved antifungal activity but possess minimal antibacterial properties in combination with fungicidal azoles. The aminoglycoside compounds are analogues of kanamycin A. Also provided are methods of synthesizing and methods of using the compounds of the present invention. The compounds of the present invention are useful in treating or preventing fungal disease.
摘要翻译: 本发明涉及新型杀真菌化合物,其包括在环III的6位上具有某些取代基的氨基糖苷类似物,其具有改善的抗真菌活性,但与杀真菌唑组合具有最小的抗菌性能。 氨基糖苷类化合物是卡那霉素A的类似物。还提供了合成方法和使用本发明化合物的方法。 本发明的化合物可用于治疗或预防真菌性疾病。
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公开(公告)号:US20050214213A1
公开(公告)日:2005-09-29
申请号:US11097315
申请日:2005-04-04
申请人: Baldomero Olivera , J. McIntosh , Maren Watkins , James Garrett , Lourdes Cruz , Michelle Grilley , Robert Schoenfeld , Craig Walker , Reshma Shetty , Robert Jones
发明人: Baldomero Olivera , J. McIntosh , Maren Watkins , James Garrett , Lourdes Cruz , Michelle Grilley , Robert Schoenfeld , Craig Walker , Reshma Shetty , Robert Jones
IPC分类号: A61K38/00 , C07K14/435 , C12N5/02 , A61K51/00 , A61K38/16
CPC分类号: C07K14/43504 , A61K38/00
摘要: The present invention is directed to conotoxin peptides, derivatives or pharmaceutically acceptable salts thereof. The present invention is further directed to the use of this peptide, derivatives thereof and pharmaceutically acceptable salts thereof for the treatment of disorders associated with voltage-gated ion channels, voltage-gated ligand channels and/or receptors. The invention is further directed to nucleic acid sequences encoding the conotoxin peptides and encoding propeptides, as well as the propeptides.
摘要翻译: 本发明涉及芋螺毒素肽,其衍生物或药学上可接受的盐。 本发明进一步涉及该肽,其衍生物和其药学上可接受的盐在治疗与电压门控离子通道,电压门控配体通道和/或受体相关的病症中的用途。 本发明还涉及编码芋螺毒素肽和编码前肽以及前肽的核酸序列。
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