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1. 发明授权

US10851174B2 Core fucosylated glycopeptides and glycoproteins: chemoenzymatic synthesis and uses thereof 有权
公开(公告)号：US10851174B2
公开(公告)日：2020-12-01
申请号：US13411733
申请日：2012-03-05
申请人： Lai-Xi Wang , Wei Huang , John Giddens
发明人： Lai-Xi Wang , Wei Huang , John Giddens
IPC分类号： C07K16/28 , C07K16/00 , C12P21/00 , C07K16/18 , C12N9/24
摘要： A chemoenzymatic method for the preparation of a core-fucoslyated glycoprotein or glycopeptide, including (a) providing an acceptor selected from the group consisting of a fucosylated GlcNAc-protein and fucosylated GlcNAc-peptide; and (b) reacting the acceptor with a donor substrate including an activated oligosaccharide moiety, in the presence of an endoglycosidase (ENGase) selected from Endo;F1, Endo-F2, Endo-F3, Endo-D and related glycosynthase mutants to transfer the oligosaccharide moiety to the acceptor and yield the structure defined core-fucosylated glycoprotein or glycopeptide. The donor substrate includes, in a specific implementation, a synthetic oligosaccharide oxazoline. A related method of fucosylated glycoprotein or fucosylated glycopeptide remodeling with a predetermined natural N-glycan or a tailor-made oligosaccharide moiety, and a method of remodeling an antibody to include a predetermined sugar chain to replace a heterogeneous sugar chain, are also described.

2. 发明申请

US20190142853A1 Inhibition of Galectin 3 Binding to the Airway Epithelial Surface to Treat or Prevent Septic Shock Resulting From Influenza and Subsequent Pneumococcal Pneumonia Infection 审中-公开
公开(公告)号：US20190142853A1
公开(公告)日：2019-05-16
申请号：US16258228
申请日：2019-01-25
申请人： Gerardo VASTA , Lai-Xi WANG
发明人： Gerardo VASTA , Lai-Xi WANG
IPC分类号： A61K31/7004 , A61P31/00 , A61K31/4192 , A61P11/00 , A61K9/107 , A61K31/351 , A61K31/7016
摘要： Galectin 3 inhibitors and methods for treating sepsis using the same are provided herein.

3. 发明授权

US07807405B2 Glycoprotein synthesis and remodeling by enzymatic transglycosylation 有权
标题翻译：糖蛋白合成和通过酶转糖基化重塑
公开(公告)号：US07807405B2
公开(公告)日：2010-10-05
申请号：US11760434
申请日：2007-06-08
申请人： Lai-Xi Wang
发明人： Lai-Xi Wang
IPC分类号： C12P21/06 , A61K39/21 , C07K1/00 , C07K1/113 , C07K14/16
CPC分类号： C07K16/00 , C07K17/10 , C12P21/005
摘要： A chemoenzymatic method for the preparation of a homogeneous glycoprotein or glycopeptide, including (a) providing an acceptor selected from the group consisting of GlcNAc-protein and GlcNAc-peptide; and (b) reacting the acceptor with a donor substrate including an activated oligosaccharide moiety, in the presence of a catalyst comprising endoglycosidase (ENGase), to transfer the oligosaccharide moiety to the acceptor and yield the homogeneous glycoprotein or glycopeptide. The donor substrate includes, in a specific implementation, a synthetic oligosaccharide oxazoline. A related method of glycoprotein or glycopeptide remodeling with a predetermined natural N-glycan or a tailor-made oligosaccharide moiety, and a method of remodeling an antibody including a heterogeneous sugar chain, are also described. The disclosed methodology enables glycoprotein drugs to be modified for prolonged half-life in vivo, reduced immunogenicity, and enhanced in vivo activity, and for targeting and drug delivery.
摘要翻译：一种用于制备均质糖蛋白或糖肽的化学酶学方法，包括（a）提供选自GlcNAc-蛋白和GlcNAc-肽的受体; 和（b）在含有糖苷内切酶（ENGase）的催化剂存在下使受体与包含活性寡糖部分的供体底物反应，将寡糖部分转移到受体并产生均质糖蛋白或糖肽。在具体实施方式中，供体底物包含合成寡糖恶唑啉。还描述了与预定的天然N-聚糖或定制寡糖部分的糖蛋白或糖肽重塑的相关方法，以及重组包含异质糖链的抗体的方法。所公开的方法使得糖蛋白药物能够在体内延长半衰期，免疫原性降低，体内活性增强，靶向和药物递送等方面进行修饰。

4. 发明申请

US20090117154A1 SYNTHETIC POLYVALENT CARBOHYDRATES AS COMPONENTS OF MICROBICIDES 审中-公开
标题翻译：合成多价碳酸酯作为微生物的组分
公开(公告)号：US20090117154A1
公开(公告)日：2009-05-07
申请号：US12066963
申请日：2006-09-14
申请人： Lai-Xi Wang , Jingsong Wang , Timothy Fouts
发明人： Lai-Xi Wang , Jingsong Wang , Timothy Fouts
IPC分类号： A61K39/21 , C12N7/00 , A61K31/715 , G01N33/566 , C08L77/00
CPC分类号： C07H3/06 , A61K31/70 , A61K31/7004 , A61K31/702 , A61K31/715 , A61K31/716 , A61K31/785 , A61K47/58 , G01N2400/10 , A61K2300/00
摘要： Inhibitors that block the DC-SIGN mediated transmission of the HIV-virus from mucosal infection sites to T-lymphocytes. In one embodiment, the inhibitors include at least one oligosaccharide chain attached to a scaffolding framework in which the number of the oligosaccharide chains attached to the scaffold can be 2, 3, 4 or more. In another embodiment, HIV-I viral infection is treated by administration of a composition including a therapeutically effective amount of an oligosaccharide cluster and/or oligosaccharide/protein cluster binding DC-SIGN, to inhibit DC-SIGN from binding to HIV envelope glycoprotein.
摘要翻译：阻断DC-SIGN介导的HIV病毒从粘膜感染部位传播到T淋巴细胞的抑制剂。在一个实施方案中，抑制剂包括连接到支架框架的至少一个寡糖链，其中附着于支架的寡糖链的数目可以是2,3,4或更多。在另一个实施方案中，通过施用包含治疗有效量的寡糖簇和/或寡糖/蛋白质簇结合DC-SIGN的组合物来治疗HIV-1病毒感染，以抑制DC-SIGN结合HIV包膜糖蛋白。

5. 发明申请

US20050176642A1 Enhancing anti-HIV efficiency through multivalent inhibitors targeting oligomeric GP120 失效
标题翻译：通过靶向寡聚GP120的多价抑制剂提高抗HIV效能
公开(公告)号：US20050176642A1
公开(公告)日：2005-08-11
申请号：US11054398
申请日：2005-02-09
申请人： Lai-Xi Wang , Hengguang Li
发明人： Lai-Xi Wang , Hengguang Li
IPC分类号： A61K31/522 , A61K31/551 , A61K31/675 , A61K38/17 , C12Q1/70 , G01N33/569
CPC分类号： G01N33/56988 , A61K31/522 , A61K31/551 , A61K31/675 , A61K38/1767 , A61K38/1774 , A61K47/55 , A61K47/62 , G01N2333/16
摘要： The present invention relates to multivalent HIV inhibitors that bind to multiple sites on a trimeric gp120 complex thereby blocking the CD4 binding site on the trimeric gp120 complex and inhibiting the attachment and entry of HIV through gp120-CD4 interactions.
摘要翻译：本发明涉及结合三聚体gp120复合物上的多个位点的多价HIV抑制剂，从而阻断三聚体gp120复合物上的CD4结合位点并抑制HIV通过gp120-CD4相互作用的附着和进入。

6. 发明申请

US20130131325A1 GLYCOPROTEIN SYNTHESIS AND REMODELING BY ENZYMATIC TRANSGLYCOSYLATION 有权
公开(公告)号：US20130131325A1
公开(公告)日：2013-05-23
申请号：US13737090
申请日：2013-01-09
申请人： LAI-XI WANG
发明人： LAI-XI WANG
IPC分类号： C07K17/10
CPC分类号： C07K16/00 , C07K17/10 , C12P21/005
摘要： A chemoenzymatic method for the preparation of a homogeneous glycoprotein or glycopeptide, including (a) providing an acceptor selected from the group consisting of GlcNAc-protein and GlcNAc-peptide; and (b) reacting the acceptor with a donor substrate including an activated oligosaccharide moiety, in the presence of a catalyst comprising endoglycosidase (ENGase), to transfer the oligosaccharide moiety to the acceptor and yield the homogeneous glycoprotein or glycopeptide. The donor substrate includes, in a specific implementation, a synthetic oligosaccharide oxazoline. A related method of glycoprotein or glycopeptide remodeling with a predetermined natural N-glycan or a tailor-made oligosaccharide moiety, and a method of remodeling an antibody including a heterogeneous sugar chain, are also described. The disclosed methodology enables glycoprotein drugs to be modified for prolonged half-life in vivo, reduced immunogenicity, and enhanced in vivo activity, and for targeting and drug delivery.

7. 发明授权

US07728106B2 HIV-1 glycopeptides and derivatives; preparation and applications thereof 失效
标题翻译： HIV-1糖肽及其衍生物; 其制备和应用
公开(公告)号：US07728106B2
公开(公告)日：2010-06-01
申请号：US11479701
申请日：2006-06-30
申请人： Lai-Xi Wang
发明人： Lai-Xi Wang
IPC分类号： C07K14/16 , C07K1/113
CPC分类号： C07K14/005 , A61K39/00 , A61K39/12 , A61K39/21 , A61K2039/6087 , A61K2039/64 , C07K1/04 , C07K9/001 , C12N2740/16122 , C12N2740/16134 , C12P21/005
摘要： A method of making a synthetic glycopeptide, by addition of a synthetic oligosaccharide oxazoline to a GlcNAc-containing peptide precursor in the presence of an enzyme selected from among Endo-A and Endo-M. In a specific implementation, the method is utilized to synthesize a trivalent V3-domain glycopeptide including three V3-domain glycopeptides on a scaffold, wherein the three V3-domain glycopeptides are arranged to mimic the V3 domain presentation in trimeric gp120. Such trivalent V3-domain glycopeptides can be utilized in a vaccine for the treatment or prevention of HIV-1 infection.
摘要翻译：通过在选自Endo-A和Endo-M的酶的存在下，向合成寡糖恶唑啉加入含GlcNAc的肽前体制备合成糖肽的方法。在具体实施方案中，该方法用于在支架上合成包含三个V3结构域糖肽的三价V3结构域糖肽，其中三个V3结构域糖肽被设置为模拟三聚体gp120中的V3结构域表达。这种三价V3结构域糖肽可用于疫苗中用于治疗或预防HIV-1感染。

8. 发明授权

US07524821B2 Scaffolded maleimide clusters for multivalent peptide assembly 有权
公开(公告)号：US07524821B2
公开(公告)日：2009-04-28
申请号：US10518108
申请日：2003-06-20
申请人： Lai-Xi Wang , Jiahong Ni , Hengguang Li , Suddham Singh
发明人： Lai-Xi Wang , Jiahong Ni , Hengguang Li , Suddham Singh
IPC分类号： A61K31/70 , A01N43/04
CPC分类号： C07D207/452 , A61K38/00 , C07D207/456 , C07J41/0055 , C07J43/003 , C07K1/1077
摘要： Disclosed are scaffolded maleimide clusters, methods of making said clusters and use of said clusters as templates for multivalent peptide assembly. Multiple maleimide functionalities were introduced onto a scaffold molecule by the reaction of a core-centered polyamines with methoxycarbonylmaleimide or with activated esters of maleimide-containing compounds. The scaffolded maleimides allow rapid, highly chemoselective, and high-yield ligation with thiolcontaining peptides under virtually neutral conditions at room temperature. The disclosed mild and highly efficient ligation method is extremely valuable for synthesizing large and complex multivalent peptides that may not be easily obtained by conventional ligation methods. These novel scaffolded maleimide clusters allow a highly chemoselective ligation with a thiolcontaining peptide under virtually neutral conditions, providing a new and efficient approach for multivalent peptide assembly. The disclosed mild and highly efficient ligation method is extremely valuable for synthesizing large and complex multivalent peptides that may not be easily obtained by conventional ligation methods. A series of multivalent peptides containing the sequence of the 36-mer HIV-1 inhibitor DP178 (T20), the T-helper epitope from tetanus toxoid (830-844), and the minimum epitope sequence of the potent HIV-neutralizing antibody 2F5 were synthesized. Carbohydrates and cholic acid were chosen as the scaffold because of their rigidity and mufti-functionality. Thus, the topology of the multivalent peptides can be controlled by the defined spatial orientation of the maleimide functionalities on the rigid scaffold core. The resulting multivalent gp41 peptides incorporating strands of DP178 on the monosaccharide and the cholic acid templates were found to be able to form three or four a-helix bundles. Moreover, the multivalent peptides containing strands of the long gp41 peptide DP178 were highly immunogenic and were able to raise high titers of peptide-specific antibodies in the absence of any additional adjuvant. Therefore, these and related multivalent peptides constructed on the maleimide clusters may be used as novel immunogens, potential inhibitors, protein mimics, artificial proteins, and powerful antigens for a broad range of biomedical applications.

9. 发明申请

US20120226024A1 CORE FUCOSYLATED GLYCOPEPTIDES AND GLYCOPROTEINS: CHEMOENZYMATIC SYNTHESIS AND USES THEREOF 审中-公开
标题翻译：核心纤维蛋白糖蛋白和糖蛋白：化学合成及其用途
公开(公告)号：US20120226024A1
公开(公告)日：2012-09-06
申请号：US13411733
申请日：2012-03-05
申请人： LAI-XI WANG , WEI HUANG , JOHN GIDDENS
发明人： LAI-XI WANG , WEI HUANG , JOHN GIDDENS
IPC分类号： C12P21/06 , C07K16/00 , C12P21/08
CPC分类号： C07K16/2887 , C07K16/00 , C07K2317/41 , C12P21/005
摘要： A chemoenzymatic method for the preparation of a core-fucoslyated glycoprotein or glycopeptide, including (a) providing an acceptor selected from the group consisting of a fucosylated GlcNAc-protein and fucosylated GlcNAc-peptide; and (b) reacting the acceptor with a donor substrate including an activated oligosaccharide moiety, in the presence of an endoglycosidase (ENGase) selected from Endo;F1, Endo-F2, Endo-F3, Endo-D and related glycosynthase mutants to transfer the oligosaccharide moiety to the acceptor and yield the structure defined core-fucosylated glycoprotein or glycopeptide. The donor substrate includes, in a specific implementation, a synthetic oligosaccharide oxazoline. A related method of fucosylated glycoprotein or fucosylated glycopeptide remodeling with a predetermined natural N-glycan or a tailor-made oligosaccharide moiety, and a method of remodeling an antibody to include a predetermined sugar chain to replace a heterogeneous sugar chain, are also described.
摘要翻译：一种用于制备核心岩藻糖化糖蛋白或糖肽的化学酶学方法，包括（a）提供选自岩藻糖基化GlcNAc蛋白和岩藻糖基化GlcNAc-肽的受体; 和（b）在选自Endo; F1，Endo-F2，Endo-F3，Endo-D和相关糖基转移酶突变体的内切糖苷酶（Engase）存在下，使受体与包含活性寡糖部分的供体底物反应，以转移寡糖部分到受体并产生结构定义的核心 - 岩藻糖基化糖蛋白或糖肽。在具体实施方式中，供体底物包含合成寡糖恶唑啉。还描述了与预定的天然N-聚糖或定制寡糖部分的岩藻糖基化糖蛋白或岩藻糖基化糖肽重塑的相关方法，以及重组抗体以包括预定糖链以取代异质糖链的方法。

10. 发明申请

US20110070607A1 GLYCOPROTEIN SYNTHESIS AND REMODELING BY ENZYMATIC TRANSGLYCOSYLATION 有权
标题翻译：糖蛋白合成和重组通过酶转移蛋白
公开(公告)号：US20110070607A1
公开(公告)日：2011-03-24
申请号：US12898284
申请日：2010-10-05
申请人： Lai-Xi Wang
发明人： Lai-Xi Wang
IPC分类号： C12P21/00 , C07K16/00 , C12N9/82 , C12N9/72 , C12N9/48 , C12N9/64 , C12N9/76 , C12N9/08
CPC分类号： C07K16/00 , C07K17/10 , C12P21/005
摘要： A chemoenzymatic method for the preparation of a homogeneous glycoprotein or glycopeptide, including (a) providing an acceptor selected from the group consisting of GlcNAc-protein and GlcNAc-peptide; and (b) reacting the acceptor with a donor substrate including an activated oligosaccharide moiety, in the presence of a catalyst comprising endoglycosidase (ENGase), to transfer the oligosaccharide moiety to the acceptor and yield the homogeneous glycoprotein or glycopeptide. The donor substrate includes, in a specific implementation, a synthetic oligosaccharide oxazoline. A related method of glycoprotein or glycopeptide remodeling with a predetermined natural N-glycan or a tailor-made oligosaccharide moiety, and a method of remodeling an antibody including a heterogeneous sugar chain, are also described. The disclosed methodology enables glycoprotein drugs to be modified for prolonged half-life in vivo, reduced immunogenicity, and enhanced in vivo activity, and for targeting and drug delivery.
摘要翻译：一种用于制备均质糖蛋白或糖肽的化学酶学方法，包括（a）提供选自GlcNAc-蛋白和GlcNAc-肽的受体; 和（b）在含有糖苷内切酶（ENGase）的催化剂存在下使受体与包含活性寡糖部分的供体底物反应，将寡糖部分转移到受体并产生均质糖蛋白或糖肽。在具体实施方式中，供体底物包含合成寡糖恶唑啉。还描述了与预定的天然N-聚糖或定制寡糖部分的糖蛋白或糖肽重塑的相关方法，以及重组包含异质糖链的抗体的方法。所公开的方法使得糖蛋白药物能够在体内延长半衰期，免疫原性降低，体内活性增强，靶向和药物递送等方面进行修饰。

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