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公开(公告)号：US20090191124A1
公开(公告)日：2009-07-30
申请号：US12336780
申请日：2008-12-17
申请人： Michael Ernest Marino , Faisal Ahmed Syud , Paul Schaffer , Brian Duh-Lan Lee , Rong Zhang , Malin Lindborg , Elin Gunneriusson , Christopher Lendel
发明人： Michael Ernest Marino , Faisal Ahmed Syud , Paul Schaffer , Brian Duh-Lan Lee , Rong Zhang , Malin Lindborg , Elin Gunneriusson , Christopher Lendel
CPC分类号： A61K51/088 , A61K49/085 , A61K49/14 , A61K51/08 , A61K51/1027 , C07K2319/00
摘要： Provided herein are PDGF-Rβ imaging agents that are polypeptides labeled with a signal generator (e.g., paramagnetic label, a radionuclide, or a fluorophore), wherein the imaging agents bind specifically to PDGFR-β. Also provided are in vivo imaging methods using the imaging agents.
摘要翻译： 本文提供PDGF-Rbeta显像剂，其是用信号发生器（例如顺磁性标记，放射性核素或荧光团）标记的多肽，其中成像剂特异性结合PDGFR-β。 还提供了使用成像剂的体内成像方法。
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公开(公告)号：US20100272641A1
公开(公告)日：2010-10-28
申请号：US12430573
申请日：2009-04-27
申请人： JACK MATHEW WEBSTER , FAISAL AHMED SYUD , BRIAN DUH-LAN LEE , PAUL SCHAFFER , RONG ZHANG , JENNIFER LYNNE HUNTINGTON , KANDE KANKANAMALAGE DAYARATHNA AMARASINGHE
发明人： JACK MATHEW WEBSTER , FAISAL AHMED SYUD , BRIAN DUH-LAN LEE , PAUL SCHAFFER , RONG ZHANG , JENNIFER LYNNE HUNTINGTON , KANDE KANKANAMALAGE DAYARATHNA AMARASINGHE
IPC分类号： A61K51/04 , C07C321/00 , C07F5/02
CPC分类号： A61K51/0406 , A61K49/0019 , A61K49/0052 , C07B59/001 , C07B2200/05 , C07C323/58 , C07C323/59 , C07F5/022
摘要： Imaging agents that comprise labeled substrates of the cystine/glutamate antiporter of cells, whereby the methods of use comprise introducing the labeled agents into cells via the cystine/glutamate antiporter, which are then reduced to a labeled cysteine, and subsequently detected in the cell.
摘要翻译： 包含细胞的胱氨酸/谷氨酸反转录酶的标记底物的成像剂，其中使用的方法包括将经标记的试剂通过胱氨酸/谷氨酸反转运体引入细胞，然后将其还原成标记的半胱氨酸，随后在细胞中检测。
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公开(公告)号：US20100143258A1
公开(公告)日：2010-06-10
申请号：US12328802
申请日：2008-12-05
申请人： Anup Sood , Jason William Castle , Evelina Roxana Loghin , Natalie Anne Staples , Kenneth Michael Fish , Randall Lee Carter , Brian Duh-Lan Lee , Kathleen Bove
发明人： Anup Sood , Jason William Castle , Evelina Roxana Loghin , Natalie Anne Staples , Kenneth Michael Fish , Randall Lee Carter , Brian Duh-Lan Lee , Kathleen Bove
CPC分类号： A61K49/0034 , A61K49/0054
摘要： In one aspect, the present invention provides a functionalized monodisperse polylysine comprising a linear monodisperse polylysine chain comprising constituent lysine monomer residues containing appended C4-C24 polyethylene glycol groups and at least one appended fluorescent dye moiety is provided.
摘要翻译： 一方面，本发明提供了包含线性单分散聚赖氨酸链的官能化单分散聚赖氨酸，其包含含有附加的C 4 -C 24聚乙二醇基团的组成赖氨酸单体残基和至少一个附加的荧光染料部分。
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公开(公告)号：US20090180954A1
公开(公告)日：2009-07-16
申请号：US12002972
申请日：2007-12-19
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.
摘要翻译： 本文提供了减少特异性结合靶标的多肽体内肝脏摄取的方法，包括：（a）提供特异性结合靶标的多肽; 和（b）用酸性氨基酸残基取代来自步骤（a）的天然多肽的至少一个碱性或至少一个中性氨基酸残基以产生修饰的多肽，其中所述修饰的多肽表现出至少0.05- 0.1个pH值小于天然多肽的等电点。 还提供了使用本发明方法制备的多肽以及采用该方法和试剂的成像技术。
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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：US20130071332A1
公开(公告)日：2013-03-21
申请号：US13234210
申请日：2011-09-16
申请人： Jack Mathew Webster , Bruce Fletcher Johnson , Brian Duh-Lan Lee , Chittari Pabba , Michael James Rishel
发明人： Jack Mathew Webster , Bruce Fletcher Johnson , Brian Duh-Lan Lee , Chittari Pabba , Michael James Rishel
CPC分类号： A61K51/0406 , C07B59/001
摘要： Imaging agents are described that comprise labeled substrates capable of being introduced into cells via the cystine/glutamate antiporter. The substrates may be used for imaging or detecting oxidative stress in cells by introducing the labeled agents into cells via the cystine/glutamate antiporter and subsequent detection.
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公开(公告)号：US08784774B2
公开(公告)日：2014-07-22
申请号：US13234210
申请日：2011-09-16
申请人： Jack Mathew Webster , Bruce Fletcher Johnson , Brian Duh-Lan Lee , Chittari Pabba , Michael James Rishel
发明人： Jack Mathew Webster , Bruce Fletcher Johnson , Brian Duh-Lan Lee , Chittari Pabba , Michael James Rishel
CPC分类号： A61K51/0406 , C07B59/001
摘要： Imaging agents are described that comprise labeled substrates capable of being introduced into cells via the cystine/glutamate antiporter. The substrates may be used for imaging or detecting oxidative stress in cells by introducing the labeled agents into cells via the cystine/glutamate antiporter and subsequent detection.
摘要翻译： 描述了包含能够通过胱氨酸/谷氨酸反向转运体引入细胞的标记底物的成像剂。 通过将标记的试剂通过胱氨酸/谷氨酸反转录酶引入细胞并随后检测，底物可用于成像或检测细胞中的氧化应激。
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公开(公告)号：US08124725B2
公开(公告)日：2012-02-28
申请号：US12336780
申请日：2008-12-17
申请人： Michael Ernest Marino , Faisal Ahmed Syud , Paul Schaffer , Brian Duh-Lan Lee , Rong Zhang , Malin Lindborg , Elin Gunneriusson , Christopher Lendel
发明人： Michael Ernest Marino , Faisal Ahmed Syud , Paul Schaffer , Brian Duh-Lan Lee , Rong Zhang , Malin Lindborg , Elin Gunneriusson , Christopher Lendel
IPC分类号： A61K38/00 , A61K49/00 , A61K38/18 , A61K51/00 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C07K14/50
CPC分类号： A61K51/088 , A61K49/085 , A61K49/14 , A61K51/08 , A61K51/1027 , C07K2319/00
摘要： Provided herein are PDGF-Rβ imaging agents that are polypeptides labeled with a signal generator (e.g., paramagnetic label, a radionuclide, or a fluorophore), wherein the imaging agents bind specifically to PDGFR-β. Also provided are in vivo imaging methods using the imaging agents.
摘要翻译： 本文提供的是PDGF-R＆bgr; 成像剂，其是用信号发生器（例如顺磁性标记，放射性核素或荧光团）标记的多肽，其中成像剂特异性结合PDGFR-和bgr。 还提供了使用成像剂的体内成像方法。
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公开(公告)号：US20090274623A1
公开(公告)日：2009-11-05
申请号：US12022526
申请日：2008-01-30
申请人： Clifford L. Smith , Faisal Ahmed Syud , Brian Duh-Lan Lee , Matthew Sam Morrison , Michael Ernest Marino , Jason William Castle , Paul Schaffer , Gabriele Matschiner , Andreas Hohlbaum , Martin Huelsmeyer , Stefan Trentmann
发明人： Clifford L. Smith , Faisal Ahmed Syud , Brian Duh-Lan Lee , Matthew Sam Morrison , Michael Ernest Marino , Jason William Castle , Paul Schaffer , Gabriele Matschiner , Andreas Hohlbaum , Martin Huelsmeyer , Stefan Trentmann
CPC分类号： A61K49/0002 , A61K49/0032 , A61K49/0056 , A61K51/088 , C07K14/47
摘要： Provided are in vivo imaging agents comprising muteins of hTLc having detectable binding affinity for c-Met or a domain thereof, coupled to a signal generator, and the mutein coupled to a signal generator is disposed in a pharmaceutically acceptable carrier. Also provided are diagnostic methods using in vivo imaging agents comprising muteins of hTLc having detectable binding affinity for c-Met or a domain thereof.
摘要翻译： 提供了包含偶联到信号发生器的具有对c-Met或其结构域的可检测结合亲和力的hTLc的突变蛋白的体内成像剂，并且耦合到信号发生器的突变蛋白置于药学上可接受的载体中。 还提供了使用体内成像剂的诊断方法，其包含对c-Met或其结构域具有可检测的结合亲和力的hTLc的突变蛋白。
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10.发明授权公开(公告)号：US08834839B2
公开(公告)日：2014-09-16
申请号：US12430573
申请日：2009-04-27
申请人： Paul Schaffer , Brian Duh-Lan Lee , Kande Kankanamalage Dayarathna Amarasinghe , Faisal Ahmed Syud , Rong Zhang , Jack Mathew Webster , Jennifer Lynne Huntington
发明人： Paul Schaffer , Brian Duh-Lan Lee , Kande Kankanamalage Dayarathna Amarasinghe , Faisal Ahmed Syud , Rong Zhang , Jack Mathew Webster , Jennifer Lynne Huntington
IPC分类号： A61K51/04 , C07C323/59 , C07B59/00 , A61K49/00 , C07C323/58 , C07F5/02
CPC分类号： A61K51/0406 , A61K49/0019 , A61K49/0052 , C07B59/001 , C07B2200/05 , C07C323/58 , C07C323/59 , C07F5/022
摘要： Imaging agents that comprise labeled substrates of the cystine/glutamate antiporter of cells, whereby the methods of use comprise introducing the labeled agents into cells via the cystine/glutamate antiporter, which are then reduced to a labeled cysteine, and subsequently detected in the cell.
摘要翻译： 包含细胞的胱氨酸/谷氨酸反转录酶的标记底物的成像剂，其中使用的方法包括将经标记的试剂通过胱氨酸/谷氨酸反转运体引入细胞，然后将其还原成标记的半胱氨酸，随后在细胞中检测。
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