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1. 发明申请

US20110064651A1 RECOMBINANT NUCLEOTIDE SEQUENCE, CELL OR VECTOR CONTAINING THE SAME AND METHOD FOR USING CELL CONTAINING THE SAME TO ENCODE ANTI-POLYETHYLENE GLYCOL MONOCLONAL ANTIBODIES 有权
标题翻译：重组核酸序列，含有该重组核苷酸序列的细胞或载体以及使用含有其的细胞编码抗聚乙二醇单克隆抗体的方法
公开(公告)号：US20110064651A1
公开(公告)日：2011-03-17
申请号：US12766930
申请日：2010-04-26
申请人： Tian-Lu Cheng , Steve R. Roffler , Kuo-Hsiang Chuang
发明人： Tian-Lu Cheng , Steve R. Roffler , Kuo-Hsiang Chuang
IPC分类号： A61K51/00 , C07H21/04 , C12N15/63 , C12N5/00 , C12P21/00 , A61K49/00 , A61B10/00
CPC分类号： A61K49/0054 , A61K49/0019 , A61K49/0032 , A61K49/186 , A61K51/065 , B82Y5/00
摘要： The invention provides a recombinant nucleotide sequence, including the sequence of SEQ ID No. 1, SEQ ID No. 2, SEQ ID No. 3 or SEQ ID No. 4, wherein the recombinant nucleotide sequence encodes an anti-polyethylene glycol recombinant single chain membrane antibody.
摘要翻译：本发明提供重组核苷酸序列，其包括SEQ ID No.1，SEQ ID No.2，SEQ ID No.3或SEQ ID No.4的序列，其中重组核苷酸序列编码抗聚乙二醇重组单链膜抗体。

2. 发明授权

US09353140B2 BQC-G, a tumor-selective anti-cancer prodrug 有权
标题翻译： BQC-G，肿瘤选择性抗癌前药
公开(公告)号：US09353140B2
公开(公告)日：2016-05-31
申请号：US13512255
申请日：2010-11-24
申请人： Zeljko M. Prijovic , Yu-Lin Leu , Steve R. Roffler
发明人： Zeljko M. Prijovic , Yu-Lin Leu , Steve R. Roffler
IPC分类号： A61K31/706 , C07H15/26 , A61P35/00 , C07H15/203
CPC分类号： C07H15/203
摘要： The invention relates to the synthesis of a second-generation camptothecin glucuronide prodrug (BQC-G) of a potent anticancer camptothecin derivative 5,6-dihydro-4H-benzo[de]quinoline-camptothecin (BQC). BQC-G was over 4000 times more water soluble than BQC, displayed good stability in human plasma and was an excellent substrate for enzymatic hydrolysis by bacterial and human β-glucuronidases. BQC-G was about 30 times less toxic than BQC, but was as toxic as BQC after hydrolysis of the glucuronide moiety by β-glucuronidase. In the presence of human serum albumin, BQC-G displayed lower cytotoxicity (IC50=1080 nM) but could be activated by β-glucuronidase to display potent activity (IC50=13.3 nM).
摘要翻译：本发明涉及有效的抗癌喜树碱衍生物5,6-二氢-4H-苯并[de]喹啉 - 喜树碱（BQC）的第二代喜树碱葡糖苷酸前药（BQC-G）的合成。 BQC-G比BQC水溶液超过4000倍，在人血浆中表现出良好的稳定性，是细菌和人类 - 葡萄糖醛酸酶进行酶水解的优良底物。 BQC-G的毒性比BQC低约30倍，但与葡萄糖醛酸苷酶部分水解后，BQC毒性相当。在人血清白蛋白存在下，BQC-G显示出更低的细胞毒性（IC50 = 1080nM），但可以被β-葡糖醛酸糖苷酶活化以显示有效活性（IC50 = 13.3nM）。

3. 发明授权

US08507207B2 Recombinant nucleotide sequence, cell or vector containing the same and method for using cell containing the same to encode anti-polyethylene glycol monoclonal antibodies 有权
标题翻译：重组核苷酸序列，含有该重组核苷酸序列的细胞或载体以及使用含有该重组核苷酸序列的细胞编码抗聚乙二醇单克隆抗体的方法
公开(公告)号：US08507207B2
公开(公告)日：2013-08-13
申请号：US12766930
申请日：2010-04-26
申请人： Tian-Lu Cheng , Steve R. Roffler , Kuo-Hsiang Chuang
发明人： Tian-Lu Cheng , Steve R. Roffler , Kuo-Hsiang Chuang
IPC分类号： G01N33/53 , C12Q1/68 , C12N15/64 , C12N15/00 , C07H21/04
CPC分类号： A61K49/0054 , A61K49/0019 , A61K49/0032 , A61K49/186 , A61K51/065 , B82Y5/00
摘要： The invention provides a recombinant nucleotide sequence, including the sequence of SEQ ID No. 1, SEQ ID No. 2, SEQ ID No. 3 or SEQ ID No. 4, wherein the recombinant nucleotide sequence encodes an anti-polyethylene glycol recombinant single chain membrane antibody.
摘要翻译：本发明提供重组核苷酸序列，其包括SEQ ID No.1，SEQ ID No.2，SEQ ID No.3或SEQ ID No.4的序列，其中重组核苷酸序列编码抗聚乙二醇重组单链膜抗体。

4. 发明申请

US20150377887A1 IN SITU AFFINITY MATURATION OF ANTIBODIES 审中-公开
标题翻译：抗原的初步研究成果
公开(公告)号：US20150377887A1
公开(公告)日：2015-12-31
申请号：US14769294
申请日：2014-02-27
申请人： Yu-cheng SU , Steve R. ROFFLER , ACADEMIA SINICA
发明人： Yu-Cheng Su , Steve R. ROFFLER
IPC分类号： G01N33/577 , C07K16/40 , C07K16/44 , G01N33/68 , G01N33/50
CPC分类号： G01N33/577 , C07K16/00 , C07K16/40 , C07K16/44 , C07K2317/14 , G01N33/5008 , G01N33/6854
摘要： This disclosure relates to a method to mimicking the germinal center reaction to generate antibodies with altered binding properties or increased affinity directly in hybridomas. To allow convenient and rapid affinity maturation of antibodies, a controllable activation-induced cytidine deaminase (AID) expression system to induce somatic hypermutation in hybridomas is developed. Selection of high affinity antibodies is achieved by fluorescence-activated cell sorting of hybridomas that preferentially bind fluorescence-labeled antigens. The disclosure also relates to de novo generation of hybridomas with tunable antibody affinity by generating myeloma fusion partners with controllable AID expression.
摘要翻译：本公开涉及模拟生发中心反应以产生具有改变的结合特性或直接在杂交瘤中增加的亲和力的抗体的方法。为了允许抗体的方便和快速的亲和力成熟，开发了可控的活化诱导的胞苷脱氨酶（AID）表达系统以诱导杂交瘤中的体细胞超突变。通过优先结合荧光标记的抗原的杂交瘤的荧光激活细胞分选来实现高亲和力抗体的选择。本公开还涉及通过产生具有可控AID表达的骨髓瘤融合配偶体从而产生具有可调节抗体亲和力的杂交瘤。

5. 发明申请

US20130012467A1 BQC-G, A TUMOR-SELECTIVE ANTI-CANCER PRODRUG 有权
标题翻译： BQC-G，肿瘤选择性抗癌剂PRODRUG
公开(公告)号：US20130012467A1
公开(公告)日：2013-01-10
申请号：US13512255
申请日：2010-11-24
申请人： Zeljko M. Prijovic , Yu-Lin Leu , Steve R. Roffler
发明人： Zeljko M. Prijovic , Yu-Lin Leu , Steve R. Roffler
IPC分类号： A61K31/706 , A61P35/00 , C07H15/26
CPC分类号： C07H15/203
摘要： The invention relates to the synthesis of a second-generation camptothecin glucuronide prodrug (BQC-G) of a potent anticancer camptothecin derivative 5,6-dihydro-4H-benzo[de]quinoline-camptothecin (BQC). BQC-G was over 4000 times more water soluble than BQC, displayed good stability in human plasma and was an excellent substrate for enzymatic hydrolysis by bacterial and human β-glucuronidases. BQC-G was about 30 times less toxic than BQC, but was as toxic as BQC after hydrolysis of the glucuronide moiety by β-glucuronidase. In the presence of human serum albumin, BQC-G displayed lower cytotoxicity (IC50=1080 nM) but could be activated by β-glucuronidase to display potent activity (IC50=13.3 nM).
摘要翻译：本发明涉及有效的抗癌喜树碱衍生物5,6-二氢-4H-苯并[de]喹啉 - 喜树碱（BQC）的第二代喜树碱葡糖苷酸前药（BQC-G）的合成。 BQC-G比BQC水溶液超过4000倍，在人血浆中表现出良好的稳定性，是细菌和人类 - 葡萄糖醛酸酶进行酶水解的优良底物。 BQC-G的毒性比BQC低约30倍，但与葡萄糖醛酸苷酶部分水解后，BQC毒性相当。在人血清白蛋白存在下，BQC-G显示出更低的细胞毒性（IC50 = 1080nM），但可以被β-葡糖醛酸糖苷酶活化以显示有效活性（IC50 = 13.3nM）。

6. 发明授权

US06699972B1 Chimeric protein and method of controlling tumor growth using the protein 失效
标题翻译：嵌合蛋白和使用蛋白质控制肿瘤生长的方法
公开(公告)号：US06699972B1
公开(公告)日：2004-03-02
申请号：US09602263
申请日：2000-06-23
申请人： Steve R. Roffler , Kuang-Wen Liao
发明人： Steve R. Roffler , Kuang-Wen Liao
IPC分类号： A61K3800
CPC分类号： C07K16/2809 , A61K2039/505 , A61K2039/5152 , A61K2039/5156 , C07K2317/622 , C07K2319/00
摘要： A chimeric protein expressed from a transgene tranduced into a mammalian tumor cell and method of using the chimeric protein for cancer treatment. The chimeric protein comprises an effector and an anchor, which are linked by a spacer. The chimeric protein, when expressed and exposed on the tumor cell surface in vivo can activate T cells, which further lead to lysis of the tumor cells. The anti-tumor effects can be enhanced by co-expression of certain co-stimulators, such as CD80 or CD86.
摘要翻译：由转染子转染入哺乳动物肿瘤细胞的嵌合蛋白和使用该嵌合蛋白进行癌症治疗的方法。嵌合蛋白包含通过间隔物连接的效应子和锚。当在体内表达和暴露于肿瘤细胞表面时，嵌合蛋白可以激活T细胞，这进一步导致肿瘤细胞裂解。可以通过共表达某些辅助刺激剂如CD80或CD86来增强抗肿瘤作用。

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