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1.
公开(公告)号:US08097701B2
公开(公告)日:2012-01-17
申请号:US13163565
申请日:2011-06-17
CPC分类号: C07K16/00 , A61K38/1825 , A61K38/215 , A61K38/37 , A61K38/45 , A61K39/00 , C07K1/006 , C07K1/1072 , C07K1/13 , C07K14/00 , C07K14/35 , C07K14/565 , C07K16/46 , C07K2317/24 , C07K2317/40 , C07K2317/52 , C07K2317/622 , C12N9/13 , C12N9/96 , C12P21/00 , C12P21/005 , C12Y208/02
摘要: The invention features compositions and methods for site-specific modification of proteins by incorporation of an aldehyde tag. Enzymatic modification at a sulfatase motif of the aldehyde tag through action of a formylglycine generating enzyme (FGE) generates a formylglycine (FGly) residue. The aldehyde moiety of FGly residue can be exploited as a chemical handle for site-specific attachment of a moiety of interest to a polypeptide.
摘要翻译: 本发明的特征在于通过掺入醛标记蛋白的位点特异性修饰的组合物和方法。 通过甲酰甘氨酸生成酶(FGE)的作用,在醛标记的硫酸酯酶基序上进行酶促修饰产生甲酰甘氨酸(FGly)残基。 FGly残基的醛部分可以用作化学处理,用于将目标部分的位点特异性连接到多肽。
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2.
公开(公告)号:US08349910B2
公开(公告)日:2013-01-08
申请号:US13163574
申请日:2011-06-17
CPC分类号: C07K16/00 , A61K38/1825 , A61K38/215 , A61K38/37 , A61K38/45 , A61K39/00 , C07K1/006 , C07K1/1072 , C07K1/13 , C07K14/00 , C07K14/35 , C07K14/565 , C07K16/46 , C07K2317/24 , C07K2317/40 , C07K2317/52 , C07K2317/622 , C12N9/13 , C12N9/96 , C12P21/00 , C12P21/005 , C12Y208/02
摘要: The invention features compositions and methods for site-specific modification of proteins by incorporation of an aldehyde tag. Enzymatic modification at a sulfatase motif of the aldehyde tag through action of a formylglycine generating enzyme (FGE) generates a formylglycine (FGly) residue. The aldehyde moiety of FGly residue can be exploited as a chemical handle for site-specific attachment of a moiety of interest to a polypeptide.
摘要翻译: 本发明的特征在于通过掺入醛标记蛋白的位点特异性修饰的组合物和方法。 通过甲酰甘氨酸生成酶(FGE)的作用,在醛标记的硫酸酯酶基序上进行酶促修饰产生甲酰甘氨酸(FGly)残基。 FGly残基的醛部分可以用作化学处理,用于将目标部分的位点特异性连接到多肽。
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公开(公告)号:US08431558B2
公开(公告)日:2013-04-30
申请号:US12049034
申请日:2008-03-14
申请人: Carolyn Ruth Bertozzi , Nicholas J. Agard , Jennifer A. Prescher , Jeremy Michael Baskin , Ellen May Sletten
发明人: Carolyn Ruth Bertozzi , Nicholas J. Agard , Jennifer A. Prescher , Jeremy Michael Baskin , Ellen May Sletten
IPC分类号: A61K31/33
CPC分类号: A61K31/655 , C07C45/292 , C07C45/511 , C07C45/63 , C07C49/457 , C07C49/753 , C07C57/26 , C07C59/72 , C07C63/66 , C07C63/74 , C07C69/708 , C07C69/76 , C07C2601/18 , C07D207/416 , C07D207/452 , C07D249/16 , C07D495/04 , G01N33/531 , G01N33/6803 , G01N33/6842 , C07C49/573
摘要: The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
摘要翻译: 本发明提供改性环炔化合物; 以及这些化合物在修饰生物分子中的使用方法。 本发明的特征在于可以在生理条件下进行的环加成反应。 通常,本发明涉及使改性的环炔与靶生物分子上的叠氮化物部分反应,产生共价修饰的生物分子。 反应的选择性及其与水性环境的相容性使其在体内(例如,在细胞表面或细胞内)和体外(例如,肽和其它聚合物的合成,生物修饰(例如,标记的)氨基酸 )。
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公开(公告)号:US08076496B2
公开(公告)日:2011-12-13
申请号:US13043274
申请日:2011-03-08
IPC分类号: C07C247/00 , C07C233/00 , G01N33/53
CPC分类号: C07K1/1077 , C07F9/5022 , C07F9/6506 , C07F9/65522 , C07F9/6561 , C07H7/02 , C07H13/00 , C07H15/203 , C07H15/26 , C07K1/023 , C07K1/04 , C07K1/1075
摘要: The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
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5.
公开(公告)号:US20130244267A1
公开(公告)日:2013-09-19
申请号:US13605695
申请日:2012-09-06
IPC分类号: C07D495/04 , C07D249/12 , C07C245/04 , C07C69/76 , C07D339/06 , C07D249/04 , C07C49/76 , C07C69/013 , C12N5/071 , G01N33/50 , C07D225/02 , C07F15/04 , C07C49/04
CPC分类号: C07D249/12 , C07C49/04 , C07C49/76 , C07C69/013 , C07C69/76 , C07C245/04 , C07C255/46 , C07C323/16 , C07C323/56 , C07C323/64 , C07C2101/14 , C07D225/02 , C07D249/04 , C07D339/06 , C07D405/12 , C07D495/04 , C07F15/045 , C12N5/0602 , G01N33/5005
摘要: The present disclosure features a strain-promoted [2+2+2] reaction that can be carried out under physiological conditions. In general, the reaction involves reacting a pi-electrophile with a low lying LUMO with a quadricyclane on a biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo and in vitro. The reaction is compatible with modification of living cells. In certain embodiments, the pi-electrophile can comprise a molecule of interest that is desired for delivery to a quadricyclane-containing biomolecule via [2+2+2] reaction.
摘要翻译: 本公开的特征在于可以在生理条件下进行的应变促进的[2 + 2 + 2]反应。 通常,该反应包括使pi-亲电子试剂与低位LUMO与生物分子上的四环体反应,产生共价修饰的生物分子。 反应的选择性及其与水性环境的相容性使其在体内和体外的应用。 该反应与活细胞的修饰相容。 在某些实施方案中,所述亲电子试剂可以包含通过[2 + 2 + 2]反应递送至含有四环素的生物分子所需的目标分子。
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公开(公告)号:US20080214801A1
公开(公告)日:2008-09-04
申请号:US11874548
申请日:2007-10-18
IPC分类号: C07H5/06 , C07F9/02 , C07D235/02 , C07C229/00
CPC分类号: C07K1/1077 , C07F9/5022 , C07F9/6506 , C07F9/65522 , C07F9/6561 , C07H7/02 , C07H13/00 , C07H15/203 , C07H15/26 , C07K1/023 , C07K1/04 , C07K1/1075
摘要: The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
摘要翻译: 本发明的特征在于可以在生理条件下进行的化学选择性连接反应。 通常,本发明涉及特异性改造的膦的缩合,其可以提供在两个反应性配对物之间形成酰胺键,产生包含膦部分的最终产物,或者可被工程化以包含可切割连接体,使得 将膦的取代基转移到叠氮化物中,释放氧化的膦副产物并在最终产物中产生天然酰胺键。 反应的选择性及其与水性环境的相容性在体内(例如,在细胞表面或细胞内)和体外(例如,肽和其他聚合物的合成,修饰(例如,标记的)氨基酸的产生 )。
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7.
公开(公告)号:US09556195B2
公开(公告)日:2017-01-31
申请号:US13605695
申请日:2012-09-06
IPC分类号: C07F15/04 , C07D495/04 , C07D249/12 , C07C245/04 , C07C69/76 , C07D339/06 , C07C49/04 , C07C49/76 , C07C69/013 , C12N5/071 , G01N33/50 , C07D225/02 , C07D249/04 , C07C323/16 , C07C323/56 , C07C323/64
CPC分类号: C07D249/12 , C07C49/04 , C07C49/76 , C07C69/013 , C07C69/76 , C07C245/04 , C07C255/46 , C07C323/16 , C07C323/56 , C07C323/64 , C07C2101/14 , C07D225/02 , C07D249/04 , C07D339/06 , C07D405/12 , C07D495/04 , C07F15/045 , C12N5/0602 , G01N33/5005
摘要: The present disclosure features a strain-promoted [2+2+2] reaction that can be carried out under physiological conditions. In general, the reaction involves reacting a pi-electrophile with a low lying LUMO with a quadricyclane on a biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo and in vitro. The reaction is compatible with modification of living cells. In certain embodiments, the pi-electrophile can comprise a molecule of interest that is desired for delivery to a quadricyclane-containing biomolecule via [2+2+2] reaction.
摘要翻译: 本公开的特征在于可以在生理条件下进行的应变促进的[2 + 2 + 2]反应。 通常,该反应包括使pi-亲电子试剂与低位LUMO与生物分子上的四环体反应,产生共价修饰的生物分子。 反应的选择性及其与水性环境的相容性使其在体内和体外的应用。 该反应与活细胞的修饰相容。 在某些实施方案中,所述亲电子试剂可以包含通过[2 + 2 + 2]反应递送至含有四环素的生物分子所需的目标分子。
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公开(公告)号:US20140199239A1
公开(公告)日:2014-07-17
申请号:US13695988
申请日:2011-05-16
申请人: Carolyn Ruth Bertozzi , Andreas Stahl , Amy Helene Henkin , Elena A. Dubikovskaya , Allison Cohen
发明人: Carolyn Ruth Bertozzi , Andreas Stahl , Amy Helene Henkin , Elena A. Dubikovskaya , Allison Cohen
CPC分类号: A61K49/0052 , A61K51/0453 , A61K51/0482 , C07D257/02 , C07D277/28 , C07D277/64 , C07D417/04 , C07D487/04 , C12Q1/66
摘要: The present disclosure provides lipid-probe compounds, and compositions comprising the compounds. A subject lipid-probe compound is useful for various imaging applications, which are also provided.
摘要翻译: 本公开提供了脂质 - 探针化合物和包含该化合物的组合物。 主题脂质 - 探针化合物对于也提供的各种成像应用是有用的。
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公开(公告)号:US08519122B2
公开(公告)日:2013-08-27
申请号:US13024908
申请日:2011-02-10
IPC分类号: C07D225/04
CPC分类号: G01N33/5005 , C07D225/08 , C07D413/06 , C07D413/14 , C07D417/06 , C07D495/04 , G01N33/532
摘要: Provided are modified cycloalkyne compounds; and methods of use of such compounds in modifying biomolecules. Embodiments include a cycloaddition reaction that can be carried out under physiological conditions. The cycloaddition reaction involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo and in vitro.
摘要翻译: 提供改性环炔化合物; 以及这些化合物在修饰生物分子中的使用方法。 实施方案包括可以在生理条件下进行的环加成反应。 环加成反应包括使修饰的环炔与靶生物分子上的叠氮化物部分反应,产生共价修饰的生物分子。 反应的选择性及其与水性环境的相容性使其在体内和体外应用。
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公开(公告)号:US20110236930A1
公开(公告)日:2011-09-29
申请号:US13043274
申请日:2011-03-08
CPC分类号: C07K1/1077 , C07F9/5022 , C07F9/6506 , C07F9/65522 , C07F9/6561 , C07H7/02 , C07H13/00 , C07H15/203 , C07H15/26 , C07K1/023 , C07K1/04 , C07K1/1075
摘要: The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
摘要翻译: 本发明的特征在于可以在生理条件下进行的化学选择性连接反应。 通常,本发明涉及特异性改造的膦的缩合,其可以提供在两个反应性配对物之间形成酰胺键,产生包含膦部分的最终产物,或者可被工程化以包含可切割连接体,使得 将膦的取代基转移到叠氮化物中,释放氧化的膦副产物并在最终产物中产生天然酰胺键。 反应的选择性及其与水性环境的相容性在体内(例如,在细胞表面或细胞内)和体外(例如,肽和其他聚合物的合成,修饰(例如,标记的)氨基酸的产生 )。
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