会员体验
专利管家（专利管理）
工作空间（专利管理）
风险监控（情报监控）
数据分析（专利分析）
侵权分析（诉讼无效）
联系我们
交流群
官方交流：
QQ群： 891211   
微信请扫码    >>>
现在联系顾问~
下载
著录项
PDF全文
热词
    • 1. 发明申请
      US20080112946A1 Catalytically active recombinant memapsin and methods of use thereof 失效
    • Catalytically active recombinant memapsin and methods of use thereof
    • 催化活性重组膜突触蛋白及其使用方法
    • US20080112946A1
    • 2008-05-15
    • US11888920
    • 2007-08-03
    • Gerald Koelsch , Jordan J. N. Tang , Lin Hong , Arun K. Ghosh , Xinli Lin
    • Gerald Koelsch , Jordan J. N. Tang , Lin Hong , Arun K. Ghosh , Xinli Lin
    • A61K38/46 , C12N9/52 , C12P21/04
    • C07K5/1021 , A61K38/00 , A61K39/00 , C07K1/1136 , C07K5/06026 , C07K5/06043 , C07K5/0806 , C07K2299/00 , C12N9/6421 , C12N9/6478 , Y02A90/26 , Y10S514/879
    • Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1). The inhibition constant of OM99-2 is 1.6×10−9 M against recombinant pro-memapsin 2. Crystallography of memapsin 2 bond to this inhibitor was used to determine the three dimensional structure of the protein, as well as the importance of the various residues in binding. This information can be used by those skilled in the art to design new inhibitors, using commercially available software programs and techniques familiar to those in organic chemistry and enzymology, to design new inhibitors to memapsin 2, useful in diagnostics and for the treatment and/or prevention of Alzheimer's disease.
    • 已经开发了用于生产纯化的，催化活性的重组突变蛋白2的方法。 已经确定了催化活性酶的底物和亚位点特异性。 底物和亚位点特异性信息用于设计可以抑制膜蛋白2功能的天然memapsin 2底物的底物类似物。底物类似物基于肽序列，显示与memapsin 2的天然肽底物相关。 底物类似物含有至少一个酰胺键的类似物，该类似物不能被膜蛋白2切割。开发了两个底物类似物合成的关键氨基酸残基位点处的等位基因，底物类似物OMR99- 1和OM99-2。 OM99-2基于由过渡态等电位羟基亚乙基取代的Leu-Ala肽键的八肽Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe（SEQ ID NO：28）（图1 ）。 OM99-2的抑制常数相对于重组前体蛋白2是1.6×10 -9 M。使用与该抑制剂的膜蛋白2键的结晶学来确定蛋白质的三维结构，以及 各种残留物在结合中的重要性。 本领域技术人员可以使用本信息来设计新的抑制剂，使用商业上可获得的有机化学和酶学方面熟悉的软件程序和技术来设计新的抑制剂2，可用于诊断和治疗和/或 预防阿尔茨海默病。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 2. 发明授权
      US07829669B2 Catalytically active recombinant memapsin and methods of use thereof 失效
    • Catalytically active recombinant memapsin and methods of use thereof
    • 催化活性重组膜突触蛋白及其使用方法
    • US07829669B2
    • 2010-11-09
    • US11888920
    • 2007-08-03
    • Gerald Koelsch , Jordan J. N. Tang , Lin Hong , Arun K. Ghosh , Xinli Lin
    • Gerald Koelsch , Jordan J. N. Tang , Lin Hong , Arun K. Ghosh , Xinli Lin
    • C07K1/00
    • C07K5/1021 , A61K38/00 , A61K39/00 , C07K1/1136 , C07K5/06026 , C07K5/06043 , C07K5/0806 , C07K2299/00 , C12N9/6421 , C12N9/6478 , Y02A90/26 , Y10S514/879
    • Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1). The inhibition constant of OM99-2 is 1.6×10−9 M against recombinant pro-memapsin 2. Crystallography of memapsin 2 bond to this inhibitor was used to determine the three dimensional structure of the protein, as well as the importance of the various residues in binding. This information can be used by those skilled in the art to design new inhibitors, using commercially available software programs and techniques familiar to those in organic chemistry and enzymology, to design new inhibitors to memapsin 2, useful in diagnostics and for the treatment and/or prevention of Alzheimer's disease.
    • 已经开发了用于生产纯化的，催化活性的重组突变蛋白2的方法。 已经确定了催化活性酶的底物和亚位点特异性。 底物和亚位点特异性信息用于设计可以抑制膜蛋白2功能的天然memapsin 2底物的底物类似物。底物类似物基于肽序列，显示与memapsin 2的天然肽底物相关。 底物类似物含有至少一个酰胺键的类似物，该类似物不能被膜蛋白2切割。开发了两个底物类似物合成的关键氨基酸残基位点处的等位基因，底物类似物OMR99- 1和OM99-2。 OM99-2基于由过渡态等电位羟基亚乙基取代的Leu-Ala肽键的八肽Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe（SEQ ID NO：28）（图1 ）。 OM99-2的抑制常数为1.6×10-9M，与重组前胶原蛋白2相似。蛋白2的结构与该抑制剂结合使用，用于测定蛋白质的三维结构，以及各种残基的重要性 绑定。 本领域技术人员可以使用本信息来设计新的抑制剂，使用商业上可获得的有机化学和酶学方面熟悉的软件程序和技术来设计新的抑制剂2，可用于诊断和治疗和/或 预防阿尔茨海默病。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 3. 发明授权
      US06545127B1 Catalytically active recombinant memapsin and methods of use thereof 失效
    • Catalytically active recombinant memapsin and methods of use thereof
    • 催化活性重组膜突触蛋白及其使用方法
    • US06545127B1
    • 2003-04-08
    • US09604608
    • 2000-06-27
    • Jordan J. N. Tang , Xinli Lin , Gerald Koelsch , Lin Hong
    • Jordan J. N. Tang , Xinli Lin , Gerald Koelsch , Lin Hong
    • G01N3348
    • C07K5/1021 , A61K38/00 , A61K39/00 , C07K1/1136 , C07K5/06026 , C07K5/06043 , C07K5/0806 , C07K2299/00 , C12N9/6421 , C12N9/6478 , Y02A90/26 , Y10S514/879
    • Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1). The inhibition constant of OM99-2 is 1.6×10−9M against recombinant pro-memapsin 2. Crystallography of memapsin 2 bound to this inhibitor was used to determine the three dimensional structure of the protein, as well as the importance of the various residues in binding. This information can be used by those skilled in the art to design new inhibitors, using commercially available software programs and techniques familiar to those in organic chemistry and enzymology, to design new inhibitors to memapsin 2, useful in diagnostics and for the treatment and/or prevention of Alzheimer's disease.
    • 已经开发了用于生产纯化的，催化活性的重组突变蛋白2的方法。 已经确定了催化活性酶的底物和亚位点特异性。 底物和亚位点特异性信息用于设计可以抑制膜蛋白2功能的天然memapsin 2底物的底物类似物。底物类似物基于肽序列，显示与memapsin 2的天然肽底物相关。 底物类似物含有至少一个酰胺键的类似物，该类似物不能被膜蛋白2切割。开发了两个底物类似物合成的关键氨基酸残基位点处的等位基因，底物类似物OMR99- 1和OM99-2。 OM99-2基于由过渡态等电位羟基亚乙基取代的Leu-Ala肽键的八肽Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe（SEQ ID NO：28）（图1 ）。 OM99-2的抑制常数为1.6×10 -9 M，与重组pro-memapsin2结合使用与此抑制剂结合的胶原蛋白2的结晶学，以确定蛋白质的三维结构，以及各种残基在结合中的重要性 。 本领域技术人员可以使用本信息来设计新的抑制剂，使用商业上可获得的有机化学和酶学方面熟悉的软件程序和技术来设计新的抑制剂2，可用于诊断和治疗和/或 预防阿尔茨海默病。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 6. 发明授权
      US06969731B1 Protease inhibitors that overcome drug resistance 失效
    • Protease inhibitors that overcome drug resistance
    • 克服耐药性的蛋白酶抑制剂
    • US06969731B1
    • 2005-11-29
    • US09506988
    • 2000-02-18
    • Jordan J. N. Tang , Arun K. Ghosh
    • Jordan J. N. Tang , Arun K. Ghosh
    • A61K31/34 , C07D307/02 , C07D307/20
    • C07D307/20
    • HIV protease inhibitors are among the most powerful drugs in suppressing HIV in human patients. However, HIV developed resistance to all protease inhibitor drugs so far marketed or used in clinical trials. HIV generates resistance by mutating its protease. The strains of HIV containing mutant proteases less vulnerable to inhibitor drug are able to replicate better and maintain the infection. No effective principle exists for the design of resistance-proof HIV protease inhibitors (HIVPr). A new inhibitor has been developed based on a new concept for designing resistance invulnerable HIVPr inhibitors. In vitro data have shown that this inhibitor is effective against many known HIVPr mutants resistant to other HIVPr inhibitor drugs. The new concept is, therefore, generally applicable for the design of other resistance invulnerable HIVPr inhibitor drugs.
    • 艾滋病毒蛋白酶抑制剂是人类抑制艾滋病毒最强大的药物之一。 然而，艾滋病毒对所有蛋白酶抑制剂药物迄今在市场上销售或用于临床试验中产生了抵抗力 HIV通过突变其蛋白酶产生抗性。 含有不易受抑制剂药物突变的蛋白酶的HIV菌株能够更好地复制并维持感染。 没有有效的原则设计耐药HIV蛋白酶抑制剂（HIVPr）。 已经开发出一种新的抑制剂，其基础是设计抗性不可抗拒的HIVPr抑制剂的新概念。 体外数据显示，该抑制剂对许多已知的对其它HIVPr抑制剂药物有抗性的HIVPr突变体是有效的。 因此，新概念通常适用于其他抗性不可抗拒的HIVPr抑制剂药物的设计。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 7. 发明授权
      US07678760B2 Inhibitors of Memapsin 2 and use thereof 失效
    • Inhibitors of Memapsin 2 and use thereof
    • Memapsin 2抑制剂及其用途
    • US07678760B2
    • 2010-03-16
    • US11763342
    • 2007-06-14
    • Jordan J. N. Tang , Arun K. Ghosh
    • Jordan J. N. Tang , Arun K. Ghosh
    • A61K38/00 , C07K16/00
    • C07K5/1021 , A61K38/00 , A61K39/00 , C07K1/1136 , C07K5/06026 , C07K5/06043 , C07K5/0806 , C07K2299/00 , C12N9/6421 , C12N9/6478 , Y02A90/26 , Y10S514/879
    • Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1). The inhibition constant of OM99-2 is 1.6×10−9 M against recombinant pro-memapsin 2. Crystallography of memapsin 2 bound to this inhibitor was used to determine the three dimensional structure of the protein, as well as the importance of the various residues in binding. This information can be used by those skilled in the art to design new inhibitors, using commercially available software programs and techniques familiar to those in organic chemistry and enzymology, to design new inhibitors to memapsin 2, useful in diagnostics and for the treatment and/or prevention of Alzheimer's disease.
    • 已经开发了用于生产纯化的，催化活性的重组突变蛋白2的方法。 已经确定了催化活性酶的底物和亚位点特异性。 底物和亚位点特异性信息用于设计可以抑制膜蛋白2功能的天然memapsin 2底物的底物类似物。底物类似物基于肽序列，显示与memapsin 2的天然肽底物相关。 底物类似物含有至少一个酰胺键的类似物，该类似物不能被膜蛋白2切割。开发了两个底物类似物合成的关键氨基酸残基位点处的等位基因，底物类似物OMR99- 1和OM99-2。 OM99-2基于由过渡态等电位羟基亚乙基取代的Leu-Ala肽键的八肽Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe（SEQ ID NO：28）（图1 ）。 OM99-2的抑制常数为1.6×10-9M，与重组pro-memapsin2结合使用与此抑制剂结合的胶原蛋白2的结晶学，以确定蛋白质的三维结构，以及各种残基的重要性 绑定。 本领域技术人员可以使用本信息来设计新的抑制剂，使用商业上可获得的有机化学和酶学方面熟悉的软件程序和技术来设计新的抑制剂2，可用于诊断和治疗和/或 预防阿尔茨海默病。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
每页展示10个专利
每页展示10个专利
每页展示20个专利
每页展示50个专利
每页展示100个专利

IPRDB

最新中国发明专利 最新美国发明专利 技术领域 专利库 专利分类库 国际专利分类库

热门服务

会员版试用 API 数据接口 找代理 知嘟嘟专利交易 排行榜 大学排行榜 专利百科

关于我们

平台介绍 战略合作 网站地图

友情链接

知嘟嘟专利交易 国家知识产权局 中国商标网

联系方式


©2019-2023 上海吉码数字技术有限公司 版权所有，并保留所有权利 沪ICP备20016256号-6 沪公网安备31011702005475号