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公开(公告)号：US20090163426A1
公开(公告)日：2009-06-25
申请号：US12323380
申请日：2008-11-25
CPC分类号： C07K5/06104 , A61K38/00 , A61K47/65 , C07K5/0819 , C07K5/1021 , C07K7/06 , G01N33/57434
摘要： The invention provides novel peptide prodrugs which contain cleavage sites specifically cleaved by prostate specific membrane antigen (PSMA). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. PSMA is secreted by prostatic glandular cells. Upon cleavage of the prodrug by PSMA, the therapeutic drugs are activated and exert their toxicity. Sesquiterpene-γ-lactones form part of the prodrugs, and are designed to be linked to carrier moieties such as the peptides of the invention. Methods for treating cell proliferative disorders are also featured in the invention.
摘要翻译： 本发明提供新的肽前体药物，其含有由前列腺特异性膜抗原（PSMA）特异性切割的切割位点。 这些前药可用于基本上抑制各种治疗药物的非特异性毒性。 PSMA由前列腺细胞分泌。 通过PSMA裂解前药时，治疗药物被活化并发挥其毒性。 倍半萜-γ-内酯形成前药的一部分，并被设计为与载体部分例如本发明的肽连接。 治疗细胞增殖性疾病的方法也在本发明中。
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公开(公告)号：US08957016B2
公开(公告)日：2015-02-17
申请号：US13485595
申请日：2012-05-31
申请人： Samuel R. Denmeade , John T. Isaacs
发明人： Samuel R. Denmeade , John T. Isaacs
CPC分类号： A61K38/08 , A61K38/168 , A61K47/65 , C07K7/06
摘要： The instant invention provides compositions comprising a prodrug, the prodrug comprising a therapeutically active drug; and a peptide selected from the group consisting of the sequences: Ser-Ser-Lys-Tyr-Gln (SEQ ID NO:1); Gly-Lys-Ser-Gln-Tyr-Gln (SEQ ID NO:2); and Gly-Ser-Ala-Lys-Tyr-Gln (SEQ ID NO:3) wherein the peptide is linked to the therapeutically active drug to inhibit the therapeutic activity of the drug, and wherein the therapeutically active drug is cleaved from the peptide upon proteolysis by an enzyme having a proteolytic activity of prostate specific antigen (PSA). The invention further provides methods of making and using the claimed compositions.
摘要翻译： 本发明提供包含前药的组合物，前药包含治疗活性药物; 和选自以下序列的肽：Ser-Ser-Lys-Tyr-Gln（SEQ ID NO：1）; Gly-Lys-Ser-Gln-Tyr-Gln（SEQ ID NO：2）; 和Gly-Ser-Ala-Lys-Tyr-Gln（SEQ ID NO：3），其中所述肽与治疗活性药物连接以抑制药物的治疗活性，并且其中治疗活性药物从肽切割 通过具有前列腺特异性抗原（PSA）的蛋白水解活性的酶进行蛋白水解。 本发明还提供制备和使用所要求保护的组合物的方法。
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公开(公告)号：US20110245147A1
公开(公告)日：2011-10-06
申请号：US12987409
申请日：2011-01-10
申请人： Samuel R. Denmeade , John T. Isaacs , Hans Lilja
发明人： Samuel R. Denmeade , John T. Isaacs , Hans Lilja
CPC分类号： C07K14/4748 , A61K38/00 , A61K47/62 , C07K7/06 , C07K14/47
摘要： The invention provides novel peptide prodrugs that contain cleavage sites specifically cleaved by human kallikrein 2 (hK2). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. Upon cleavage of the prodrug by hK2, the therapeutic drugs are activated and exert their toxicity. Methods for treating cell proliferative disorders are also featured in the invention.
摘要翻译： 本发明提供新的肽前体药物，其含有由人激肽释放酶2（hK2）特异性切割的切割位点。 这些前药可用于基本上抑制各种治疗药物的非特异性毒性。 当通过hK2裂解前体药物时，治疗药物被活化并发挥其毒性。 治疗细胞增殖性疾病的方法也在本发明中。
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4.发明授权Proaerolysin containing protease activation sequences and methods of use for treatment of prostate cancer 有权含有蛋白酶活化序列的原溶蛋白和用于治疗前列腺癌的方法公开(公告)号：US07838266B2
公开(公告)日：2010-11-23
申请号：US12788913
申请日：2010-05-27
IPC分类号： A61K38/16 , C07K14/195 , C07K19/00 , C12N15/62
CPC分类号： A61K39/0011 , A61K38/00 , C07K14/195 , C07K14/32 , C07K14/325 , C07K14/33 , C07K2319/00 , C12N9/52
摘要： Disclosed herein are modified proaerolysin (PA) peptide. In some examples, the proteins include a prostate-specific protease cleavage site and can further include a prostate-tissue-specific binding domain which functionally replaces the native PA binding domain. In other examples, the proteins include a furin cleavage site and a prostate tissue-specific binding domain which functionally replaces the native PA binding domain. Methods of using such peptides to treat prostate cancer are also disclosed.
摘要翻译： 本文公开了修饰的原胶溶素（PA）肽。 在一些实例中，蛋白质包括前列腺特异性蛋白酶切割位点，并且可以进一步包括在功能上替代天然PA结合结构域的前列腺组织特异性结合结构域。 在其他实例中，蛋白质包括弗林蛋白酶切割位点和功能性替代天然PA结合结构域的前列腺组织特异性结合结构域。 还公开了使用这些肽治疗前列腺癌的方法。
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公开(公告)号：US08450280B2
公开(公告)日：2013-05-28
申请号：US13473356
申请日：2012-05-16
申请人： Samuel R. Denmeade , John T. Isaacs , Hans Lilja
发明人： Samuel R. Denmeade , John T. Isaacs , Hans Lilja
CPC分类号： C12N9/6445 , A61K47/65 , C07K7/06 , C07K14/47
摘要： The invention provides novel peptide prodrugs that contain cleavage sites specifically cleaved by human kallikrein 2 (hK2). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. Upon cleavage of the prodrug by hK2, the therapeutic drugs are activated and exert their toxicity. Methods for treating cell proliferative disorders are also featured in the invention.
摘要翻译： 本发明提供新的肽前体药物，其含有由人激肽释放酶2（hK2）特异性切割的切割位点。 这些前药可用于基本上抑制各种治疗药物的非特异性毒性。 当通过hK2裂解前体药物时，治疗药物被活化并发挥其毒性。 治疗细胞增殖性疾病的方法也在本发明中。
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公开(公告)号：US07635682B2
公开(公告)日：2009-12-22
申请号：US11328491
申请日：2006-01-06
申请人： Samuel R. Denmeade , John T. Isaacs
发明人： Samuel R. Denmeade , John T. Isaacs
IPC分类号： A61K49/00
CPC分类号： A61K38/08 , A61K38/168 , A61K47/65 , C07K7/06
摘要： The instant invention provides compositions comprising a prodrug, the prodrug comprising a therapeutically active drug; and a peptide selected from the group consisting of the sequences: Ser-Ser-Lys-Tyr-Gln (SEQ ID NO:1);Gly-Lys-Ser-Gln-Tyr-Gln (SEQ ID NO:2); and Gly-Ser-Ala-Lys-Tyr-Gln (SEQ ID NO:3) wherein the peptide is linked to the therapeutically active drug to inhibit the therapeutic activity of the drug, and wherein the therapeutically active drug is cleaved from the peptide upon proteolysis by an enzyme having a proteolytic activity of prostate specific antigen (PSA). The invention further provides methods of making and using the claimed compositions.
摘要翻译： 本发明提供包含前药的组合物，前药包含治疗活性药物; 和选自以下序列的肽：Ser-Ser-Lys-Tyr-Gln（SEQ ID NO：1）; Gly-Lys-Ser-Gln-Tyr-Gln（SEQ ID NO：2）; 和Gly-Ser-Ala-Lys-Tyr-Gln（SEQ ID NO：3），其中所述肽与治疗活性药物连接以抑制药物的治疗活性，并且其中治疗活性药物从肽切割 通过具有前列腺特异性抗原（PSA）的蛋白水解活性的酶进行蛋白水解。 本发明还提供制备和使用所要求保护的组合物的方法。
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公开(公告)号：US20090274625A1
公开(公告)日：2009-11-05
申请号：US12087400
申请日：2007-01-05
CPC分类号： G01N33/57492 , A61K38/00 , C07K7/08 , G01N2333/705
摘要： The instant invention provides methods and compositions for the treatment and diagnosis of cancer, e.g., cancers characterized by the expression of prostate specific membrane antigen (PSMA).
摘要翻译： 本发明提供了用于治疗和诊断癌症的方法和组合物，例如以前列腺特异性膜抗原（PSMA）表达为特征的癌症。
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公开(公告)号：US07053042B1
公开(公告)日：2006-05-30
申请号：US09627600
申请日：2000-07-28
申请人： Samuel R. Denmeade , John T. Isaacs , Hans Lilja
发明人： Samuel R. Denmeade , John T. Isaacs , Hans Lilja
CPC分类号： C12N9/6445 , C07K14/47
摘要： The invention provides novel peptide prodrugs that contain cleavage sites specifically cleaved by human kallikrein 2 (hK2). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. Upon cleavage of the prodrug by hK2, the therapeutic drugs are activated and exert their toxicity. Methods for treating cell proliferative disorders are also featured in the invention.
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公开(公告)号：US06504014B1
公开(公告)日：2003-01-07
申请号：US09588822
申请日：2000-06-07
IPC分类号： C07K1600
CPC分类号： C07D307/935 , A61K31/33 , A61K31/34 , A61K38/00 , A61K47/62 , A61K47/65 , C07D307/93 , C07K14/47
摘要： The invention provides novel peptide prodrugs which contain cleavage sites specifically cleaved by prostate specific antigen (PSA). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. PSA is secreted by prostatic glandular cells. Upon cleavage of the prodrug by PSA, the therapeutic drugs are activated and exert their toxicity. Novel sesquiterpene-&ggr;-lactones are also provided by the invention, and are designed to be linked to carrier moieties such as the peptides of the invention. Methods for treating cell proliferative disorders are also featured in the invention.
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公开(公告)号：US20120309692A1
公开(公告)日：2012-12-06
申请号：US13473356
申请日：2012-05-16
申请人： Samuel R. Denmeade , John T. Isaacs , Hans Lilja
发明人： Samuel R. Denmeade , John T. Isaacs , Hans Lilja
CPC分类号： C12N9/6445 , A61K47/65 , C07K7/06 , C07K14/47
摘要： The invention provides novel peptide prodrugs that contain cleavage sites specifically cleaved by human kallikrein 2 (hK2). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. Upon cleavage of the prodrug by hK2, the therapeutic drugs are activated and exert their toxicity. Methods for treating cell proliferative disorders are also featured in the invention.
摘要翻译： 本发明提供新的肽前体药物，其含有由人激肽释放酶2（hK2）特异性切割的切割位点。 这些前药可用于基本上抑制各种治疗药物的非特异性毒性。 当通过hK2裂解前体药物时，治疗药物被活化并发挥其毒性。 治疗细胞增殖性疾病的方法也在本发明中。
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