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1. 发明申请

WO2011008260A3 BIFUNCTIONAL STAPLED POLYPEPTIDES AND USES THEREOF 审中-公开
标题翻译：双功能固定多肽及其用途
公开(公告)号：WO2011008260A3
公开(公告)日：2011-03-24
申请号：PCT/US2010001952
申请日：2010-07-13
申请人： HARVARD COLLEGE , VERDINE GREGORY L , GROSSMANN TOM N , MOELLERING RAYMOND E , YEH JOHANNES TSUNG-HAN , LIANG YUE , OAK YOUBEAN
发明人： VERDINE GREGORY L , GROSSMANN TOM N , MOELLERING RAYMOND E , YEH JOHANNES TSUNG-HAN , LIANG YUE , OAK YOUBEAN
IPC分类号： A61K38/00
CPC分类号： C07K14/47 , A61K38/00 , A61K47/60 , A61K47/62 , A61K47/64 , A61K47/65 , A61K47/66 , C07K1/107 , C07K1/1077 , C07K1/113 , C07K14/435 , C07K14/4747 , C07K2319/00 , C07K2319/01 , C12N9/93 , C12Y603/02019 , C40B30/04
摘要： The invention relates to bifunctional stapled or stiched peptides comprising a targeting domain, a linker moiety, and an effector domain, that can be used to tether, or to bring into close proximity, at least two cellular entities (e.g., proteins). Certain aspects relate to bifunctional stapled or stiched peptides that bind to an effector biomolecule through the effector domain and bind to a target biomolecule through the targeting domain. Polypeptides and/or polypeptide complexes that are tethered by the bifunctional stapled or stiched peptides of the invention, where the effector polypeptide bound to the effector domain of the bifunctional stapled or stiched peptide modifies or alters the target polypeptide bound to the targeting domain of the bifunctional peptide. Usesses of the inventive bifunctional stapled or stiched peptides including methods for treatment of disease (e.g., cancer, inflammatory diseases) are also provided.
摘要翻译：本发明涉及包含靶向结构域，连接体部分和效应子结构域的双功能钉合或固定肽，其可以用于连接或使至少两个细胞实体（例如蛋白质）紧密接近。某些方面涉及通过效应器结构域结合效应生物分子并通过靶向结构域与靶生物分子结合的双功能钉合或固定肽。通过本发明的双功能钉扎或固定肽连接的多肽和/或多肽复合物，其中与双功能钉链或固定肽的效应子结构域结合的效应子多肽修饰或改变与双功能靶向结构域结合的靶多肽肽。还提供了包括用于治疗疾病（例如癌症，炎性疾病）的方法的本发明双功能钉合或固定肽的用途。

2. 发明申请

WO2006131749A2 SCAFFOLD 审中-公开
标题翻译：脚手架
公开(公告)号：WO2006131749A2
公开(公告)日：2006-12-14
申请号：PCT/GB2006/002115
申请日：2006-06-08
申请人： MEDICAL RESEARCH COUNCIL , WOODMAN, Robbie , YEH, Johannes, Tsung-Han , LAURENSON, Sophie , KO FERRIGNO, Paul
发明人： WOODMAN, Robbie , YEH, Johannes, Tsung-Han , LAURENSON, Sophie , KO FERRIGNO, Paul
CPC分类号： C07K14/8139 , C07K7/06 , C12N15/1044
摘要： The present invention relates to the use of Stefin A as a scaffold protein for the display of inserted peptides, particularly wherein the Stefin A is a human Stefin A. Several mutations are advantageously made in the wild type stefin A sequence to improve it as a scaffold; preferably the Stefin A comprises a heterologous peptide insertion at the Leu 73 site. Furthermore, preferably the scaffold protein comprises a V48D mutation; preferably the scaffold protein comprises a G4W mutation. Preferably the scaffold comprises Leu73, V48D and G4W mutations. The invention also relates to the scaffold proteins themselves, in particular a stefin A polypeptide having the Leu73, V48D and G4W mutations, such as shown as SEQ ID NO: 1. The invention also relates to a method for identifying binding proteins and to peptide A (RLNKPLPSLPV) and its use in treating yeast infections.
摘要翻译：本发明涉及使用Stefin A作为展示插入肽的支架蛋白，特别是其中Stefin A是人类Stefin A。有利的是在野生型stefin A序列中进行突变以改善其作为支架 ; 优选地，Stefin A包含在Leu 73位点处的异源肽插入。此外，优选地，支架蛋白包含V48D突变; 优选地，支架蛋白包含G4W突变。优选地，支架包含Leu73，V48D和G4W突变。本发明还涉及支架蛋白本身，特别是具有Leu73，V48D和G4W突变的stefin A多肽，如SEQ ID NO：1所示。本发明还涉及鉴定结合蛋白和肽A的方法（RLNKPLPSLPV）及其在治疗酵母菌感染中的应用。

3. 发明申请

WO2006131749A3 SCAFFOLD 审中-公开
标题翻译：脚手架
公开(公告)号：WO2006131749A3
公开(公告)日：2007-05-18
申请号：PCT/GB2006002115
申请日：2006-06-08
申请人： MEDICAL RES COUNCIL , WOODMAN ROBBIE , YEH JOHANNES TSUNG-HAN , LAURENSON SOPHIE , KO FERRIGNO PAUL
发明人： WOODMAN ROBBIE , YEH JOHANNES TSUNG-HAN , LAURENSON SOPHIE , KO FERRIGNO PAUL
IPC分类号： C07K14/81 , A61K38/08 , A61P31/10 , C07K7/06 , C12N15/10 , C12N15/62 , G01N33/53
CPC分类号： C07K14/8139 , C07K7/06 , C12N15/1044
摘要： The present invention relates to the use of Stefin A as a scaffold protein for the display of inserted peptides, particularly wherein the Stefin A is a human Stefin A. Several mutations are advantageously made in the wild type stefin A sequence to improve it as a scaffold; preferably the Stefin A comprises a heterologous peptide insertion at the Leu 73 site. Furthermore, preferably the scaffold protein comprises a V48D mutation; preferably the scaffold protein comprises a G4W mutation. Preferably the scaffold comprises Leu73, V48D and G4W mutations. The invention also relates to the scaffold proteins themselves, in particular a stefin A polypeptide having the Leu73, V48D and G4W mutations, such as shown as SEQ ID NO: 1. The invention also relates to a method for identifying binding proteins and to peptide A (RLNKPLPSLPV) and its use in treating yeast infections.
摘要翻译：本发明涉及使用Stefin A作为展示插入肽的支架蛋白，特别是其中Stefin A是人SteFen A.几种突变有利地在野生型stefin A序列中制成，以改善其作为支架 ; 优选地，Stefin A包含在Leu 73位点处的异源肽插入。此外，优选地，支架蛋白包含V48D突变; 优选地，支架蛋白包含G4W突变。优选地，所述支架包含Leu73，V48D和G4W突变。本发明还涉及支架蛋白本身，特别是具有Leu73，V48D和G4W突变的stefin A多肽，如SEQ ID NO：1所示。本发明还涉及鉴定结合蛋白和肽A的方法（RLNKPLPSLPV）及其在治疗酵母菌感染中的应用。

4. 发明申请

WO2012040459A2 BETA-CATENIN TARGETING PEPTIDES AND USES THEREOF 审中-公开
标题翻译： β-谷氨酸靶向肽及其用途
公开(公告)号：WO2012040459A2
公开(公告)日：2012-03-29
申请号：PCT/US2011052755
申请日：2011-09-22
申请人： HARVARD COLLEGE , VERDINE GREGORY L , GROSSMANN TOM N , YEH JOHANNES TSUNG-HAN
发明人： VERDINE GREGORY L , GROSSMANN TOM N , YEH JOHANNES TSUNG-HAN
IPC分类号： A61K38/10
CPC分类号： C07K14/4705 , A61K38/00 , C07K1/113 , C07K7/08 , C07K14/47 , C07K14/4702 , C07K14/4703
摘要： The invention relates to ß-catenin targeting peptides comprising an a-helical segment that are optionally stapled or stitched, and pharmaceutical compositions thereof. Uses of the inventive ß-catenin targeting polypeptides including methods for treatment of disease, such as diseases associated with aberrant Wnt signaling, including cancer, are also provided.
摘要翻译：本发明涉及包含可选择地缝合或缝合的α-螺旋区段的β-连环蛋白靶向肽及其药物组合物。还提供了本发明的β-连环蛋白靶向多肽的用途，包括治疗疾病的方法，例如与异常Wnt信号传导相关的疾病，包括癌症。

5. 发明申请

WO2011008260A2 BIFUNCTIONAL STAPLED POLYPEPTIDES AND USES THEREOF 审中-公开
标题翻译：双功能多功能胶囊及其用途
公开(公告)号：WO2011008260A2
公开(公告)日：2011-01-20
申请号：PCT/US2010/001952
申请日：2010-07-13
申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE , VERDINE, Gregory, L. , GROSSMANN, Tom, N. , MOELLERING, Raymond, E. , YEH, Johannes, Tsung-Han , LIANG, Yue , OAK, Youbean
发明人： VERDINE, Gregory, L. , GROSSMANN, Tom, N. , MOELLERING, Raymond, E. , YEH, Johannes, Tsung-Han , LIANG, Yue , OAK, Youbean
IPC分类号： A61K38/12 , C40B30/04
CPC分类号： C07K14/47 , A61K38/00 , A61K47/60 , A61K47/62 , A61K47/64 , A61K47/65 , A61K47/66 , C07K1/107 , C07K1/1077 , C07K1/113 , C07K14/435 , C07K14/4747 , C07K2319/00 , C07K2319/01 , C12N9/93 , C12Y603/02019 , C40B30/04
摘要： The invention relates to bifunctional stapled or stiched peptides comprising a targeting domain, a linker moiety, and an effector domain, that can be used to tether, or to bring into close proximity, at least two cellular entities (e.g., proteins). Certain aspects relate to bifunctional stapled or stiched peptides that bind to an effector biomolecule through the effector domain and bind to a target biomolecule through the targeting domain. Polypeptides and/or polypeptide complexes that are tethered by the bifunctional stapled or stiched peptides of the invention, where the effector polypeptide bound to the effector domain of the bifunctional stapled or stiched peptide modifies or alters the target polypeptide bound to the targeting domain of the bifunctional peptide. Usesses of the inventive bifunctional stapled or stiched peptides including methods for treatment of disease (e.g., cancer, inflammatory diseases) are also provided.
摘要翻译：本发明涉及可用于系链或至少两个细胞实体（例如蛋白质）紧密接近的双功能缝合或包封的肽，其包含靶向结构域，接头部分和效应结构域。某些方面涉及通过效应结构域结合到效应物生物分子并通过靶向结构域结合靶标生物分子的双功能缝合或保持肽。通过本发明的双功能缝合或紧密多肽的束缚的多肽和/或多肽复合物，其中效应子多肽与双功能性钉合或固定的肽的效应结构域结合，修饰或改变与双功能的靶向结构域结合的靶多肽肽。还提供了本发明的双功能缝合或包封肽包括治疗疾病（例如癌症，炎性疾病）的方法。

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