公开(公告)号：US20100104585A1

公开(公告)日：2010-04-29

申请号：US12571983

申请日：2009-10-01

申请人： Laura L. Kiessling ,  Byron R. Griffith ,  Jason E. Gestwicki ,  Laura Strong

发明人： Laura L. Kiessling ,  Byron R. Griffith ,  Jason E. Gestwicki ,  Laura Strong

IPC分类号： A61K39/395

CPC分类号： A61K31/70 ,  A61K31/74 ,  A61K38/178 ,  B82Y30/00 ,  G01N33/5005

摘要： Multivalent ligands which carry or display at least one recognition element (RE), and preferably a plurality of recognition elements, for binding directly or indirectly to cells or other biological particles or more generally by binding to any biological molecule. The multivalent ligands provided can function for binding or targeting to any biological particle or molecule and particularly to targeting of cells or cell types or viruses, for cell aggregation and for macromolecular assembly of biological macromolecules. The multivalent ligands of this invention are applicable for creating scaffolds (assemblies) of chemical or biological species, including without limitation, antigens, epitopes, ligand binding groups, ligands for cell receptors and various macromolecules. In these scaffolds, the number, spacing, relative positioning and relative orientation of recognition elements can be controlled. The invention also relates to methods for aggregating biological particles and macromolecules and for modulating biological response employing the multivalent ligands provided.

摘要翻译： 携带或显示至少一种识别元件（RE）的多价配体，并且优选多个识别元件，用于直接或间接地结合细胞或其他生物颗粒，或更一般地通过结合任何生物分子。 所提供的多价配体可用于结合或靶向任何生物颗粒或分子，特别是靶向细胞或细胞类型或病毒，用于细胞聚集和生物大分子的大分子装配。 本发明的多价配体适用于生成化学或生物物种的支架（组件），包括但不限于抗原，表位，配体结合基团，细胞受体配体和各种大分子。 在这些支架中，可以控制识别元件的数量，间距，相对定位和相对定向。 本发明还涉及聚集生物颗粒和大分子的方法以及使用所提供的多价配体来调节生物反应的方法。

公开(公告)号：US20080114157A1

公开(公告)日：2008-05-15

申请号：US11850877

申请日：2007-09-06

申请人： Jon S. Thorson ,  Byron R. Griffith

发明人： Jon S. Thorson ,  Byron R. Griffith

IPC分类号： C07K14/00

CPC分类号： C07K9/008

摘要： The present invention generally relates to methods and compositions for generating vancomycin analogs. Specifically the invention relates to generating a vancomycin library through chemoselective ligation of a sugar moiety with a vancomycin aglycon. In particular, the present invention provides a library of vancomycin analogs, where the member of the library comprises at least one vancomycin analog selected from 2′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 3′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 4′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 6′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 2′-N-acylbiphenyl-glucosyl vancomycin neoglycoside, 3′-N-acylbiphenoyl-glucosyl vancomycin neoglycoside, 4′-N-acylbiphenoyl-glucosyl vancomycin neoglycoside and 6′-N-acylbiphenoyl-glucosyl vancomycin neoglycoside.

摘要翻译： 本发明一般涉及用于产生万古霉素类似物的方法和组合物。 具体地，本发明涉及通过糖部分与万古霉素苷元的化学选择性连接产生万古霉素文库。 特别地，本发明提供了万古霉素类似物的文库，其中文库的成员包含至少一种选自2'-N-酰基癸酰基 - 葡糖基万古霉素新糖苷，3'- N-酰基癸酰基 - 葡糖基万古霉素新糖苷，4 'N-酰基癸酰基 - 葡萄糖基万古霉素新糖苷，6'-N-酰基癸酰基 - 葡萄糖基万古霉素新糖苷，2'- N-酰基联苯 - 葡萄糖基万古霉素新糖苷，3'- N-酰基联苯酰基 - 葡萄糖基万古霉素新糖苷，4'-N-酰基联苯酰基 - 葡萄糖基万古霉素新糖苷和6'-N-酰基联苯酰基 - 葡萄糖基万古霉素新糖苷。

公开(公告)号：US20130030151A1

公开(公告)日：2013-01-31

申请号：US13544329

申请日：2012-07-09

申请人： Jon S. Thorson ,  Byron R. Griffith

发明人： Jon S. Thorson ,  Byron R. Griffith

IPC分类号： C07K9/00

CPC分类号： C07K9/008

摘要： The present invention generally relates to methods and compositions for generating vancomycin analogs. Specifically the invention relates to generating a vancomycin library through chemoselective ligation of a sugar moiety with a vancomycin aglycon. In particular, the present invention provides a library of vancomycin analogs, where the member of the library comprises at least one vancomycin analog selected from 2′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 3′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 4′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 6′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 2′-N-acylbiphenyl-glucosyl vancomycin neoglycoside, 3′-N-acylbiphenoyl-glucosyl vancomycin neoglycoside, 4′-N-acylbiphenoyl-glucosyl vancomycin neoglycoside and 6′-N-acylbiphenoyl-glucosyl vancomycin neoglycoside.

摘要翻译： 本发明一般涉及用于产生万古霉素类似物的方法和组合物。 具体地，本发明涉及通过糖部分与万古霉素苷元的化学选择性连接产生万古霉素文库。 特别地，本发明提供了万古霉素类似物的文库，其中文库的成员包含至少一种选自2'-N-酰基癸酰基 - 葡糖基万古霉素新糖苷，3'- N-酰基癸酰基 - 葡糖基万古霉素新糖苷，4 'N-酰基癸酰基 - 葡萄糖基万古霉素新糖苷，6'-N-酰基癸酰基 - 葡萄糖基万古霉素新糖苷，2'- N-酰基联苯 - 葡萄糖基万古霉素新糖苷，3'- N-酰基联苯酰基 - 葡萄糖基万古霉素新糖苷，4'-N-酰基联苯酰基 - 葡萄糖基万古霉素新糖苷和6'-N-酰基联苯酰基 - 葡萄糖基万古霉素新糖苷。

公开(公告)号：US20090275485A1

公开(公告)日：2009-11-05

申请号：US11847731

申请日：2007-08-30

申请人： Jon S. Thorson ,  Changsgeng Zhang ,  Byron R. Griffith

发明人： Jon S. Thorson ,  Changsgeng Zhang ,  Byron R. Griffith

IPC分类号： C40B50/06 ,  C12P19/60 ,  C12P19/44 ,  C07H17/08

CPC分类号： C12P19/623 ,  C07H15/203 ,  C07H17/08 ,  C07H19/01 ,  C07K9/008 ,  C12P19/18 ,  C12P19/44 ,  C12P19/62

摘要： The present invention relates to methods of use of glycosyltransferases and related novel compounds. The invention exploits the reversibility of glycosyltransferases to generate new sugars, unnatural biomolecules and numerous one-pot reactions for generation of new biomolecules having varied backbones such as enediynes, vancomycins, bleomycins, anthracyclines, macrolides, pluramycins, aureolic acids, indolocarbazoles, aminglycosides, glycopeptides, polyenes, coumarins, benzoisochromanequinones, calicheamicins, erythromycin, avermectins, ivermectins, angucyclines, cardiac glycosides, steroids or flavinoids. In preferred embodiments, the invention specifically relates to biosynthesis of anticancer (the enediyne calicheamicin, CLM), anthelmintic agents (the macrolides avermectin, ivermectin and erythromycin) and antibiotic (the glycopeptide vancomycin, VCM) natural product-based drugs developed by reversible, bidirectional glycosyltransferase-catalyzed reactions.

摘要翻译： 本发明涉及使用糖基转移酶和相关新化合物的方法。 本发明利用糖基转移酶的可逆性来产生新的糖，非天然生物分子和许多一锅反应，用于产生具有不同骨架的新的生物分子，例如恩多奈斯 ，多烯，香豆素，苯并二叠氮醌，加利车霉素，红霉素，阿凡曼菌素，伊维来菌素，角叉菜苷，强心苷，类固醇或黄素类。 在优选的实施方案中，本发明特别涉及抗逆转（双胍），抗胆碱药物（大环内酯阿维菌素，伊维菌素和红霉素）和抗生素（甘氨酸万古霉素，VCM）基于天然产物的药物的生物合成 糖基转移酶催化反应。

公开(公告)号：US08710182B2

公开(公告)日：2014-04-29

申请号：US13544329

申请日：2012-07-09

申请人： Jon S. Thorson ,  Byron R. Griffith

发明人： Jon S. Thorson ,  Byron R. Griffith

IPC分类号： C07K9/00

CPC分类号： C07K9/008

摘要： The present invention generally relates to methods and compositions for generating vancomycin analogs. Specifically the invention relates to generating a vancomycin library through chemoselective ligation of a sugar moiety with a vancomycin aglycon. In particular, the present invention provides a library of vancomycin analogs, where the member of the library comprises at least one vancomycin analog selected from 2′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 3′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 4′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 6′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 2′-N-acylbiphenyl-glucosyl vancomycin neoglycoside, 3′-N-acylbiphenoyl-glucosyl vancomycin neoglycoside, 4′-N-acylbiphenoyl-glucosyl vancomycin neoglycoside and 6′-N-acylbiphenoyl-glucosyl vancomycin neoglycoside.

摘要翻译： 本发明一般涉及用于产生万古霉素类似物的方法和组合物。 具体地，本发明涉及通过糖部分与万古霉素苷元的化学选择性连接产生万古霉素文库。 特别地，本发明提供了万古霉素类似物的文库，其中文库的成员包含至少一种选自2'-N-酰基癸酰基 - 葡糖基万古霉素新糖苷，3'- N-酰基癸酰基 - 葡糖基万古霉素新糖苷，4 'N-酰基癸酰基 - 葡萄糖基万古霉素新糖苷，6'-N-酰基癸酰基 - 葡萄糖基万古霉素新糖苷，2'- N-酰基联苯 - 葡萄糖基万古霉素新糖苷，3'- N-酰基联苯酰基 - 葡萄糖基万古霉素新糖苷，4'-N-酰基联苯酰基 - 葡萄糖基万古霉素新糖苷和6'-N-酰基联苯酰基 - 葡萄糖基万古霉素新糖苷。

公开(公告)号：US08841092B2

公开(公告)日：2014-09-23

申请号：US11847731

申请日：2007-08-30

申请人： Jon S. Thorson ,  Changsgeng Zhang ,  Byron R. Griffith

发明人： Jon S. Thorson ,  Changsgeng Zhang ,  Byron R. Griffith

IPC分类号： C12P19/38 ,  C12P19/00 ,  C12P19/18 ,  C07H19/01 ,  C07H15/203 ,  C07H17/08 ,  C07K9/00 ,  C12P19/44 ,  C12P19/62

CPC分类号： C12P19/623 ,  C07H15/203 ,  C07H17/08 ,  C07H19/01 ,  C07K9/008 ,  C12P19/18 ,  C12P19/44 ,  C12P19/62

摘要： The present invention relates to methods of use of glycosyltransferases and related compounds. The invention exploits the reversibility of glycosyltransferases to generate new sugars, unnatural biomolecules and numerous one-pot reactions for generation of new biomolecules having varied backbones such as enediynes, vancomycins, bleomycins, anthracyclines, macrolides, pluramycins, aureolic acids, indolocarbazoles, aminglycosides, glycopeptides, polyenes, coumarins, benzoisochromanequinones, calicheamicins, erythromycin, avermectins, ivermectins, angucyclines, cardiac glycosides, steroids or flavinoids. In preferred embodiments, the invention specifically relates to biosynthesis of anticancer (the enediyne calicheamicin, CLM), anthelmintic agents (the macrolides avermectin, ivermectin and erythromycin) and antibiotic (the glycopeptide vancomycin, VCM) natural product-based drugs developed by reversible, bidirectional glycosyltransferase-catalyzed reactions.

摘要翻译： 本发明涉及使用糖基转移酶和相关化合物的方法。 本发明利用糖基转移酶的可逆性来产生新的糖，非天然生物分子和许多一锅反应，用于产生具有不同骨架的新的生物分子，所述新生物分子具有不同的骨架，例如恩二烯，万古霉素，博来霉素，蒽环类抗生素，大环内酯类，阿拉伯霉素，阿拉伯酸，吲哚糖苷， ，多烯，香豆素，苯并二叠氮醌，加利车霉素，红霉素，阿凡曼菌素，伊维来菌素，角叉菜苷，强心苷，类固醇或黄素类。 在优选的实施方案中，本发明特别涉及抗逆转（双胍），抗胆碱药物（大环内酯阿维菌素，伊维菌素和红霉素）和抗生素（甘氨酸万古霉素，VCM）基于天然产物的药物的生物合成 糖基转移酶催化反应。

公开(公告)号：US08236926B2

公开(公告)日：2012-08-07

申请号：US11850877

申请日：2007-09-06

申请人： Jon S. Thorson ,  Byron R. Griffith

发明人： Jon S. Thorson ,  Byron R. Griffith

IPC分类号： C07K14/00

CPC分类号： C07K9/008

摘要： The present invention generally relates to methods and compositions for generating vancomycin analogs. Specifically the invention relates to generating a vancomycin library through chemoselective ligation of a sugar moiety with a vancomycin aglycon. In particular, the present invention provides a library of vancomycin analogs, where the member of the library comprises at least one vancomycin analog selected from 2′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 3′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 4′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 6′-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 2′-N-acylbiphenyl-glucosyl vancomycin neoglycoside, 3′-N-acylbiphenoyl-glucosyl vancomycin neoglycoside, 4′-N-acylbiphenoyl-glucosyl vancomycin neoglycoside and 6′-N-acylbiphenoyl-glucosyl vancomycin neoglycoside.

摘要翻译： 本发明一般涉及用于产生万古霉素类似物的方法和组合物。 具体地，本发明涉及通过糖部分与万古霉素苷元的化学选择性连接产生万古霉素文库。 特别地，本发明提供了万古霉素类似物的文库，其中文库的成员包含至少一种选自2'-N-酰基癸酰基 - 葡糖基万古霉素新糖苷，3'- N-酰基癸酰基 - 葡糖基万古霉素新糖苷，4 'N-酰基癸酰基 - 葡萄糖基万古霉素新糖苷，6'-N-酰基癸酰基 - 葡萄糖基万古霉素新糖苷，2'- N-酰基联苯 - 葡萄糖基万古霉素新糖苷，3'- N-酰基联苯酰基 - 葡萄糖基万古霉素新糖苷，4'-N-酰基联苯酰基 - 葡萄糖基万古霉素新糖苷和6'-N-酰基联苯酰基 - 葡萄糖基万古霉素新糖苷。