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公开(公告)号：US08501909B2
公开(公告)日：2013-08-06
申请号：US12735068
申请日：2008-12-22
CPC分类号： A61K51/08 , A61K38/00 , A61K51/088 , C07K16/32
摘要： HER2 binding polypeptides comprising the amino acid sequence EX1 RNAYWEIA LLPNLTNQQK RAFIRKLYDD PSQSSELLX2E AKKLNDSQ wherein X1 in position 2 is M, I or L, and X2 in position 39 is S or C (SEQ ID NO: 1) are disclosed. Moreover, such peptides comprising a chelating environment are disclosed. Also radiolabeled polypeptides formed by the peptides comprising a chelating environment and radionuclides are disclosed. Furthermore, methods of in vivo imaging of the body of a mammalian subject having or suspected of having a cancer characterized by overexpression of HER2 comprising administration of such a radiolabeled polypeptide followed by obtainment of an image of the body using a medical imaging instrument and also methods of treating such cancer are disclosed. Furthermore, the use of such a radiolabeled polypeptide in diagnosis and treatment of cancer characterized by overexpression of HER2. Nucleic acids encoding the polypeptides, expression vectors comprising the nucleic acids and host cells comprising the expression vectors are also disclosed.
摘要翻译： HER2结合多肽包含氨基酸序列EX1 RNAYWEIA LLPNLTNQQK RAFIRKLYDD PSQSSELLX2E AKKLNDSQ，其中位置2中的X1是M，I或L，而位置39的X2是S或C（SEQ ID NO：1）。 此外，公开了包含螯合环境的这些肽。 还公开了由包含螯合环境和放射性核素的肽形成的放射性标记的多肽。 此外，具有或怀疑具有HER2过表达的哺乳动物受试者的身体的体内成像方法包括施用这种放射性标记的多肽，然后使用医学成像仪获得身体的图像，以及方法 公开了治疗这种癌症的方法。 此外，这种放射性标记的多肽在诊断和治疗HER2过表达的癌症中的应用。 还公开了编码多肽的核酸，包含核酸的表达载体和包含表达载体的宿主细胞。
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公开(公告)号：US20110020223A1
公开(公告)日：2011-01-27
申请号：US12735068
申请日：2008-12-22
CPC分类号： A61K51/08 , A61K38/00 , A61K51/088 , C07K16/32
摘要： HER2 binding polypeptides comprising the amino acid sequence EX1 RNAYWEIA LLPNLTNQQK RAFIRKLYDD PSQSSELLX2E AKKLNDSQ wherein X1 in position 2 is M, I or L, and X2 in position 39 is S or C (SEQ ID NO:1) are disclosed. Moreover, such peptides comprising a chelating environment are disclosed. Also radiolabeled polypeptides formed by the peptides comprising a chelating environment and radionuclides are disclosed. Furthermore, methods of in vivo imaging of the body of a mammalian subject having or suspected of having a cancer characterized by overexpression of HER2 comprising administration of such a radiolabeled polypeptide followed by obtainment of an image of the body using a medical imaging instrument and also methods of treating such cancer are disclosed. Furthermore, the use of such a radiolabeled polypeptide in diagnosis and treatment of cancer characterized by overexpression of HER2. Nucleic acids encoding the polypeptides, expression vectors comprising the nucleic acids and host cells comprising the expression vectors are also disclosed.
摘要翻译： HER2结合多肽包含氨基酸序列EX1 RNAYWEIA LLPNLTNQQK RAFIRKLYDD PSQSSELLX2E AKKLNDSQ，其中位置2中的X1是M，I或L，而位置39的X2是S或C（SEQ ID NO：1）。 此外，公开了包含螯合环境的这些肽。 还公开了由包含螯合环境和放射性核素的肽形成的放射性标记的多肽。 此外，具有或怀疑具有HER2过表达的哺乳动物受试者的身体的体内成像方法包括施用这种放射性标记的多肽，然后使用医学成像仪获得身体的图像，以及方法 公开了治疗这种癌症的方法。 此外，这种放射性标记的多肽在诊断和治疗HER2过表达的癌症中的应用。 还公开了编码多肽的核酸，包含核酸的表达载体和包含表达载体的宿主细胞。
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公开(公告)号：US09469670B2
公开(公告)日：2016-10-18
申请号：US12735069
申请日：2008-12-22
CPC分类号： C07K14/31 , C07K1/047 , C12N15/1037 , C12N15/1041 , C12N15/1044 , C12N15/1075 , C40B40/10 , G01N33/6845 , G01N2333/31
摘要： Populations of polypeptide variants based on a common scaffold, each polypeptide in the population comprising the scaffold amino acid sequence EXXXAXXEIX XLPNLTXXQX XAFIXKLXDD PSQSSELLSE AKKLNDSQ (SEQ ID NO: 1) or AKYAKEXXXAXX EIXXLPNLTX XQXXAFIXKL XDDPSQSSEL LSEAKKLNDS Q (SEQ ID NO:2), wherein each X individually corresponds to an amino acid residue which is varied in the population are disclosed. Also populations of polynucleotides, wherein each member encodes a member of a polypeptide population are disclosed. Furthermore, combinations of such polypeptide populations and such polynucleotide populations are disclosed, wherein each member of polypeptide population is physically or spatially associated with the polynucleotide encoding that member via means for genotype-phenotype coupling.
摘要翻译： 基于共同支架的多肽变体群体，群体中的每个多肽包含支架氨基酸序列EXXXAXXEIX XLPNLTXXQX XAFIXKLXDD PSQSSELLSE AKKLNDSQ（SEQ ID NO：1）或AKYAKEXXXAXX EIXXLPNLTX XQXXAFIXKL XDDPSQSSEL LSEAKKLNDS Q（SEQ ID NO：2），其中每个 X分别对应于在群体中变化的氨基酸残基。 还公开了多核苷酸的种群，其中每个成员编码多肽群体的成员。 此外，公开了这种多肽群体和这种多核苷酸群体的组合，其中多肽群体的每个成员通过用于基因型 - 表型偶联的方式与编码该成员的多核苷酸物理或空间相关联。
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公开(公告)号：US20100286366A1
公开(公告)日：2010-11-11
申请号：US12735069
申请日：2008-12-22
CPC分类号： C07K14/31 , C07K1/047 , C12N15/1037 , C12N15/1041 , C12N15/1044 , C12N15/1075 , C40B40/10 , G01N33/6845 , G01N2333/31
摘要： Populations of polypeptide variants based on a common scaffold, each polypeptide in the population comprising the scaffold amino acid sequence EXXXAXXEIX XLPNLTXXQX XAFIXKLXDD PSQSSELLSE AKKLNDSQ or AKYAKEXXXAXX EIXXLPNLTX XQXXAFIXKL XDDPSQSSEL LSEAKKLNDS Q, wherein each X individually corresponds to an amino acid residue which is varied in the population are disclosed. Also populations of polynucleotides, wherein each member encodes a member of a polypeptide population are disclosed. Furthermore, combinations of such polypeptide populations and such polynucleotide populations are disclosed, wherein each member of polypeptide population is physically or spatially associated with the polynucleotide encoding that member via means for genotype-phenotype coupling. Furthermore, methods for selecting a desired polypeptide having an affinity for a predetermined target from a population of polypeptides, isolation of a polynucleotide encoding a desired polypeptide having an affinity for a predetermined target, identifying a desired polypeptide having an affinity for a predetermined target, selecting and identifying a desired polypeptide having affinity for a predetermined target, and production of a desired polypeptide having an affinity for a predetermined target are disclosed.
摘要翻译： 基于常见支架的多肽变体群体，群体中的每个多肽包含支架氨基酸序列EXXXAXXEIX XLPNLTXXQX XAFIXKLXDD PSQSSELLSE AKKLNDSQ或AKYAKEXXXAXX EIXXLPNLTX XQXXAFIXKL XDDPSQSSEL LSEAKKLNDS Q，其中每个X分别对应于在群体中变化的氨基酸残基 被披露。 还公开了多核苷酸的种群，其中每个成员编码多肽群体的成员。 此外，公开了这种多肽群体和这种多核苷酸群体的组合，其中多肽群体的每个成员通过用于基因型 - 表型偶联的方式与编码该成员的多核苷酸物理或空间相关联。 此外，从多肽群体中选择对预定靶标具有亲和性的期望多肽的方法，分离编码对预定靶标具有亲和性的期望多肽的多核苷酸，鉴定对预定靶标具有亲和性的期望多肽，选择 并鉴定对预定靶标具有亲和力的所需多肽，以及对预定靶标具有亲和性的所需多肽的制备。
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公开(公告)号：US20120165650A1
公开(公告)日：2012-06-28
申请号：US12975425
申请日：2010-12-22
申请人： Faisal Ahmed Syud , Brian Duh-Lan Lee , Rong Zhang , Peter Brian Iveson , Paul Schaffer , Tove Eriksson , Elin Gunneriusson , Fredrik Frejd , Lars Abrahmsen , Joachim Feldwisch , Nina Herne , Christofer Lendel
发明人： Faisal Ahmed Syud , Brian Duh-Lan Lee , Rong Zhang , Peter Brian Iveson , Paul Schaffer , Tove Eriksson , Elin Gunneriusson , Fredrik Frejd , Lars Abrahmsen , Joachim Feldwisch , Nina Herne , Christofer Lendel
CPC分类号： A61K51/088 , C07K14/71
摘要： Imaging agents comprising an isolated polypeptide conjugated with a radionuclide and a chelator; wherein the isolated polypeptide binds specifically to HER2, or a variant thereof; and methods for preparing and using these imaging agents.
摘要翻译： 包含与放射性核素和螯合剂缀合的分离的多肽的成像剂; 其中所述分离的多肽特异性结合HER2或其变体; 以及制备和使用这些成像剂的方法。
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公开(公告)号：US09187535B2
公开(公告)日：2015-11-17
申请号：US12735070
申请日：2008-12-17
IPC分类号： C07K14/31
CPC分类号： C07K14/31 , C07K2318/20 , C07K2319/00
摘要： The invention provides a platelet derived growth factor receptor beta (PDGF-Rβ) binding polypeptide, comprising a platelet derived growth factor receptor beta binding motif, PBM, which motif consists of an amino acid sequence as defined herein, wherein the PDGF-Rβ-binding polypeptide binds to PDGF-Rβ such that the KD value of the interaction is at most 1×10−6 M. Also provided are methods and uses of said polypeptide in treatment and diagnosis of PDGF-Rβ-related conditions.
摘要翻译： 本发明提供了一种血小板衍生生长因子受体β（PDGF-R＆bgr）结合多肽，其包含血小板衍生生长因子受体β结合基序，PBM，该基序由本文定义的氨基酸序列组成，其中PDGF-R＆bgr; 结合多肽结合PDGF-R＆bgr; 使得相互作用的KD值至多为1×10 -6 M。还提供了所述多肽在治疗和诊断PDGF-R＆bgr相关病症中的方法和用途。
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公开(公告)号：US20110021424A1
公开(公告)日：2011-01-27
申请号：US12735070
申请日：2008-12-17
IPC分类号： A61K38/16 , C07K14/31 , C07K14/00 , A61P35/02 , A61P35/04 , A61P9/12 , A61P27/02 , A61P1/16 , A61P9/00 , A61P9/10
CPC分类号： C07K14/31 , C07K2318/20 , C07K2319/00
摘要： The invention provides a platelet derived growth factor receptor beta (PDGF-Rβ) binding polypeptide, comprising a platelet derived growth factor receptor beta binding motif, PBM, which motif consists of an amino acid sequence as defined herein, wherein the PDGF-Rβ-binding polypeptide binds to PDGF-Rβ such that the KD value of the interaction is at most 1×10−6 M. Also provided are methods and uses of said polypeptide in treatment and diagnosis of PDGF-Rβ-related conditions.
摘要翻译： 本发明提供了一种血小板衍生生长因子受体β（PDGF-R＆bgr）结合多肽，其包含血小板衍生生长因子受体β结合基序，PBM，该基序由本文定义的氨基酸序列组成，其中PDGF-R＆bgr; 结合多肽结合PDGF-R＆bgr; 使得相互作用的KD值至多为1×10 -6 M。还提供了所述多肽在治疗和诊断PDGF-R＆bgr相关病症中的方法和用途。
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公开(公告)号：US09238810B2
公开(公告)日：2016-01-19
申请号：US12996260
申请日：2008-09-24
CPC分类号： C12N15/1086 , C07K14/00 , C07K14/31 , C07K17/02 , C07K2317/52
摘要： The invention provides an immunoglobulin G Fc region binding polypeptide, which polypeptide comprises an immunoglobulin G Fc region binding motif, BM, consisting of an amino acid sequence selected from: i) EQQX4AFYEILHLPNLTEX18QX20X21AFIX25X26LRX29, (SEQ ID NO:12) and ii) an amino acid sequence which has at least 85% identity to the sequence defined in i). Also provided are methods of isolation or production of IgG Fc-containing molecules.
摘要翻译： 本发明提供免疫球蛋白G Fc区结合多肽，该多肽包含免疫球蛋白G Fc区结合基序，BM，其选自：i）EQQX4AFYEILHLPNLTEX18QX20X21AFIX25X26LRX29，（SEQ ID NO：12）和ii） 序列与i）中定义的序列具有至少85％的同一性。 还提供了分离或产生含有IgG Fc的分子的方法。
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公开(公告)号：US08937047B2
公开(公告)日：2015-01-20
申请号：US12002972
申请日：2007-12-19
申请人： Michael Ernest Marino , Faisal Ahmed Syud , Jason William Castle , Brian Duh-Lan Lee , Malin Lindborg , Elin Gunneriusson , Christofer Lendel
发明人： Michael Ernest Marino , Faisal Ahmed Syud , Jason William Castle , Brian Duh-Lan Lee , Malin Lindborg , Elin Gunneriusson , Christofer Lendel
IPC分类号： A61K38/16 , A61K51/08 , A61K38/00 , C07K14/00 , A61K51/10 , C07K16/00 , C07K16/24 , C07K16/32 , C07K16/28
CPC分类号： C07K16/2863 , A61K51/1084 , A61K51/109 , C07K16/00 , C07K16/241 , C07K16/32 , C07K2318/20 , C07K2319/00
摘要： Provided herein are methods of reducing liver uptake in vivo of a polypeptide that specifically binds to a target comprising: (a) providing a polypeptide that specifically binds to a target; and (b) substituting at least one basic or at least one neutral amino acid residue of the native polypeptide from step (a) with an acidic amino acid residue to produce a modified polypeptide, wherein the modified polypeptide demonstrates an isoelectric point at least 0.05-0.1 pH points less than the isoelectric point of the native polypeptide. Also provided are polypeptides made using the inventive methods as well as imaging techniques that employ the methods and agents.
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公开(公告)号：US08426557B2
公开(公告)日：2013-04-23
申请号：US12452996
申请日：2008-07-17
申请人： Thomas Bergman , Anders Jarstad , Torbjörn Gräslund , Tove Eriksson , Andreas Jonsson , Jingjing Li , Christofer Lendel
发明人： Thomas Bergman , Anders Jarstad , Torbjörn Gräslund , Tove Eriksson , Andreas Jonsson , Jingjing Li , Christofer Lendel
摘要： This invention relates to polypeptides which bind to IGF-1R and to applications of those polypeptides in medicine, veterinary medicine, diagnostics and imaging.
摘要翻译： 本发明涉及结合IGF-1R的多肽以及这些多肽在医学，兽医学，诊断学和成像中的应用。
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