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公开(公告)号：US08343458B2
公开(公告)日：2013-01-01
申请号：US12418116
申请日：2009-04-03
申请人： Matthew S. Bogyo , Galia Blum , Alicia Berger , Zhen Cheng , Sanjiv S. Gambhir
发明人： Matthew S. Bogyo , Galia Blum , Alicia Berger , Zhen Cheng , Sanjiv S. Gambhir
CPC分类号： A61K51/08 , A61B6/508 , A61K49/0032 , A61K49/0056 , A61K51/0495 , A61K51/088
摘要： Activity-based probes, which are specific for certain active cysteine proteases (caspase, cathepsin and legumain) and carry radioactive labels, are disclosed. The present probes comprise an acyloxymethyketone (AOMK) “warhead” that binds only to active enzyme. The probes further comprise peptide-like structure that targets the probe to a specific cysteine protease or protease family, and a radiolabel on the probe, which is bound to the targeted enzyme. It has been found that the present probes are stable in vivo and give specific target images distinguishable over background. The preferred probes are labeled with a positron-emitting agent such as 64Cu, 125I (SPECT) and 99mTc (PET). The probes show in vivo half-life and stability well suited for imaging.
摘要翻译： 公开了基于活性的探针，其特异于某些活性半胱氨酸蛋白酶（半胱天冬酶，组织蛋白酶和legumain）和携带放射性标记。 本发明的探针包括只与活性酶结合的酰氧基甲基酮（AOMK）弹头。 探针进一步包含将探针靶向特定半胱氨酸蛋白酶或蛋白酶家族的肽样结构，以及与靶向酶结合的探针上的放射性标记。 已经发现本发明的探针在体内是稳定的，并且可以在背景下区分特定的目标图像。 优选的探针用正电子发射剂如64Cu，125I（SPECT）和99mTc（PET）标记。 探针显示体内半衰期和稳定性，非常适合成像。
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2.发明申请公开(公告)号：US20070036725A1
公开(公告)日：2007-02-15
申请号：US11502255
申请日：2006-08-10
申请人： Matthew Bogyo , Galia Blum , Georges von Degenfeld
发明人： Matthew Bogyo , Galia Blum , Georges von Degenfeld
CPC分类号： C07K1/1077 , A61K49/0021 , A61K49/0023 , A61K49/0032 , A61K49/0041 , A61K49/0043 , A61K49/0056 , C07K5/06078
摘要： Methods and materials for the imaging of cells containing active proteases such as cathepsin are disclosed. The present materials include activity based probes that bind to an enzyme and are subsequently cleaved. Cleavage results in a fluorescent signal due to removal of a quenching group which, when present on the probe causes altered or no fluorescence. The probes employ an acyloxymethyl ketone reactive group, one or more amino acids for determining specificity, a fluorophore and a quencher. The probes are cell permeable and may use, for example, a QSY7 (diarylyrhodamine) quencher and a BODIPY (bora-diaza-indecene) dye.
摘要翻译： 公开了用于含有活性蛋白酶如组织蛋白酶的细胞成像的方法和材料。 本发明的材料包括与酶结合并随后被切割的基于活性的探针。 切割导致荧光信号，因为去除了淬灭基团，当存在于探针上时会引起改变或无荧光。 探针使用酰氧基甲基酮反应性基团，一个或多个用于确定特异性的氨基酸，荧光团和猝灭剂。 探针是细胞可渗透的，并且可以使用例如QSY7（二元罗丹明）猝灭剂和BODIPY（硼 - 二氮杂 - 茚二烯）染料。
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公开(公告)号：US20090252677A1
公开(公告)日：2009-10-08
申请号：US12418116
申请日：2009-04-03
申请人： Matthew S. Bogyo , Galia Blum , Alicia Berger , Zhen Cheng , Sanjiv S. Gambhir
发明人： Matthew S. Bogyo , Galia Blum , Alicia Berger , Zhen Cheng , Sanjiv S. Gambhir
CPC分类号： A61K51/08 , A61B6/508 , A61K49/0032 , A61K49/0056 , A61K51/0495 , A61K51/088
摘要： Activity-based probes, which are specific for certain active cysteine proteases (caspase, cathepsin and legumain) and carry radioactive labels, are disclosed. The present probes comprise an acyloxymethyketone (AOMK) “warhead” that binds only to active enzyme. The probes further comprise peptide-like structure that targets the probe to a specific cysteine protease or protease family, and a radiolabel on the probe, which is bound to the targeted enzyme. It has been found that the present probes are stable in vivo and give specific target images distinguishable over background. The preferred probes are labeled with a positron-emitting agent such as 64Cu, 125I (SPECT) and 99mTc (PET). The probes show in vivo half-life and stability well suited for imaging.
摘要翻译： 公开了基于活性的探针，其特异于某些活性半胱氨酸蛋白酶（半胱天冬酶，组织蛋白酶和legumain）和携带放射性标记。 本发明的探针包括只与活性酶结合的酰氧基甲基酮（AOMK）“弹头”。 探针进一步包含将探针靶向特定半胱氨酸蛋白酶或蛋白酶家族的肽样结构，以及与靶向酶结合的探针上的放射性标记。 已经发现本发明的探针在体内是稳定的，并且可以在背景下区分特定的目标图像。 优选的探针用正电子发射剂如64Cu，125I（SPECT）和99mTc（PET）标记。 探针显示体内半衰期和稳定性，非常适合成像。
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4.发明授权公开(公告)号：US08968700B2
公开(公告)日：2015-03-03
申请号：US11502255
申请日：2006-08-10
CPC分类号： C07K1/1077 , A61K49/0021 , A61K49/0023 , A61K49/0032 , A61K49/0041 , A61K49/0043 , A61K49/0056 , C07K5/06078
摘要： Methods and materials for the imaging of cells containing active proteases such as cathepsin are disclosed. The present materials include activity based probes that bind to an enzyme and are subsequently cleaved. Cleavage results in a fluorescent signal due to removal of a quenching group which, when present on the probe causes altered or no fluorescence. The probes employ an acyloxymethyl ketone reactive group, one or more amino acids for determining specificity, a fluorophore and a quencher. The probes are cell permeable and may use, for example, a QSY7 (diarylyrhodamine) quencher and a BODIPY (bora-diaza-indecene) dye.
摘要翻译： 公开了用于含有活性蛋白酶如组织蛋白酶的细胞成像的方法和材料。 本发明的材料包括与酶结合并随后被切割的基于活性的探针。 切割导致荧光信号，因为去除了淬灭基团，当存在于探针上时会引起改变或无荧光。 探针使用酰氧基甲基酮反应性基团，一个或多个用于确定特异性的氨基酸，荧光团和猝灭剂。 探针是细胞可渗透的，并且可以使用例如QSY7（二元罗丹明）猝灭剂和BODIPY（硼 - 二氮杂 - 茚二烯）染料。
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公开(公告)号：US20050143430A1
公开(公告)日：2005-06-30
申请号：US10914010
申请日：2004-08-05
申请人： Aviv Gazit , Alexander Levitzki , Galia Blum
发明人： Aviv Gazit , Alexander Levitzki , Galia Blum
IPC分类号： A61K31/4184 , A61K31/423 , A61K31/424 , A61P3/00 , A61P3/10 , A61P5/00 , A61P5/50 , A61P9/00 , A61P9/10 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/04 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D235/24 , C07D263/58
CPC分类号： C07D263/58
摘要： The present invention provides catechol bioisostere compounds which are potent inhibitors of protein tyrosine kinases (PTKs). The present invention further provides methods of inhibiting PTKs, for example receptor protein tyrosine kinases (RTKs), comprising administering the catechol bioisosteres. The catechol bioisostere compounds are useful in treating or preventing PTK-related disease states, particularly protein tyrosine kinase related disorders which are associated with defects in signaling pathways mediated by PTKs.
摘要翻译： 本发明提供了作为蛋白酪氨酸激酶（PTK）的有效抑制剂的儿茶酚生物电子等排化合物。 本发明还提供了抑制PTK的方法，例如受体蛋白酪氨酸激酶（RTK），其包括施用儿茶酚生物电子等排体。 邻苯二酚生物电子等离子体化合物可用于治疗或预防PTK相关疾病状态，特别是与由PTK介导的信号传导途径缺陷相关的蛋白酪氨酸激酶相关病症。
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