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1. 发明申请

US20070015234A1 Whole cell assay for inhibitors of cathepsin k 审中-公开
标题翻译：用于组织蛋白酶k抑制剂的全细胞测定
公开(公告)号：US20070015234A1
公开(公告)日：2007-01-18
申请号：US10570925
申请日：2004-09-17
申请人： Sylvie Desmarais , Jean-Pierre Falgueyret , Christophe Mellon
发明人： Sylvie Desmarais , Jean-Pierre Falgueyret , Christophe Mellon
IPC分类号： C12Q1/37 , A61K31/655
CPC分类号： G01N33/5044 , C12Q1/37 , G01N33/60 , G01N33/6887 , G01N2500/00 , G01N2500/10
摘要： The present invention relates to a method of identifying and evaluating chemical inhibitors of cathepsin K activity in whole cells. The present invention also relates to probes that are capable of forming irreversible adducts with cathepsin K at the active site. The probes used in the instant invention comprise a radioactive functional group to allow the detection of the irreversible cathepsin K-probe adducts.
摘要翻译：本发明涉及鉴定和评价全细胞中组织蛋白酶K活性的化学抑制剂的方法。本发明还涉及能够在活性部位与组织蛋白酶K形成不可逆加合物的探针。本发明中使用的探针包括放射性官能团，以允许检测不可逆的组织蛋白酶K-探针加合物。

2. 发明授权

US6114132A Prosphatase binding assay 失效
标题翻译： Prosphatase结合测定
公开(公告)号：US6114132A
公开(公告)日：2000-09-05
申请号：US964313
申请日：1997-11-04
申请人： Sylvie Desmarais , Michael Gresser , Richard Friesen , Brian Kennedy , Don Nicholson , Kathryn Skorey , Chidambaran Ramachandran , Anthony Ford-Hutchinson
发明人： Sylvie Desmarais , Michael Gresser , Richard Friesen , Brian Kennedy , Don Nicholson , Kathryn Skorey , Chidambaran Ramachandran , Anthony Ford-Hutchinson
IPC分类号： G01N33/573 , C07K5/08 , C07K5/083 , C07K5/087 , C07K5/09 , C07K5/093 , C07K5/097 , C12N11/00 , C12N15/09 , C12Q1/34 , C12Q1/37 , C12Q1/42 , C12Q1/48 , C12N9/96
CPC分类号： G01N33/573 , C07K5/0827 , C12Q1/34 , C12Q1/37 , C12Q1/42 , G01N2333/96466
摘要： Disclosed is a binding assay for proteases and phosphatases, which contain cysteine in their binding sites or as a necessary structural component for enzymatic binding. The sulfhydryl group of cysteine is the nucleophilic group in the enzyme's mechanistic proteolytic and hydrolytic properties. The assay can be used to determine the ability of new, unknown ligands and mixtures of compounds to competitively bind with the enzyme versus a known binding agent for the enzyme, e.g., a known enzyme inhibitor. By the use of a mutant form of the natural or native wild-type enzyme, in which serine, or another amino acid, e.g., alanine, replaces cysteine, the problem of interference from extraneous oxidizing and alkylating agents in the assay procedure is overcome. The interference arises because of oxidation or alkylation of the sulfhydryl, --SH (or --S.sup.-), in the cysteine, which then adversely affects the binding ability of the enzyme. Specifically disclosed is an assay for tyrosine phosphatases and cysteine proteases, including caspases and cathepsins, e.g., Cathepsin K(O2), utilizing scintillation proximity assay (SPA) technology. The assay has important applications in the discovery of compounds for the treatment and study of, for example, diabetes, immunosuppression, cancer, Alzheimer's disease and osteoporosis. The novel feature of the use of a mutant enzyme can be extended to its use in a wide variety of conventional colorimetric, photometric, spectrophotometric, radioimmunoassay and ligand-binding competitive assays.
摘要翻译：公开了蛋白酶和磷酸酶的结合测定法，其在其结合位点含有半胱氨酸或作为酶结合的必需结构组分。半胱氨酸的巯基是酶的机理蛋白水解和水解性质中的亲核基团。该测定法可用于测定新的未知配体和化合物的混合物与酶竞争性结合的能力，与酶的已知结合剂，例如已知的酶抑制剂。通过使用天然或天然野生型酶的突变形式，其中丝氨酸或另一氨基酸例如丙氨酸取代半胱氨酸，克服了测定程序中来自外来氧化和烷化剂的干扰问题。干扰是由于半胱氨酸中巯基-SH（或-S-）的氧化或烷基化而产生的，其然后不利地影响酶的结合能力。具体公开的是利用闪烁近邻测定（SPA）技术的酪氨酸磷酸酶和半胱氨酸蛋白酶的测定法，包括胱天蛋白酶和组织蛋白酶，例如组织蛋白酶K（O 2）。该测定在发现用于治疗和研究例如糖尿病，免疫抑制，癌症，阿尔茨海默氏病和骨质疏松症的化合物中具有重要应用。使用突变酶的新颖特征可以扩展到其在各种常规比色，光度，分光光度，放射免疫测定和配体结合竞争性测定中的用途。

3. 发明授权

US06348572B1 Ligands for phosphatase binding assay 失效
标题翻译：用于磷酸酶结合测定的配体
公开(公告)号：US06348572B1
公开(公告)日：2002-02-19
申请号：US09069138
申请日：1998-04-29
申请人： Sylvie Desmarais , Robert Zamboni , Richard Friesen , Yves LeBlanc , Claude Dufresne , Robert N. Young , Patrick Roy
发明人： Sylvie Desmarais , Robert Zamboni , Richard Friesen , Yves LeBlanc , Claude Dufresne , Robert N. Young , Patrick Roy
IPC分类号： C07K508
CPC分类号： G11B7/244 , G11B7/247 , G11B7/25
摘要： Disclosed are new ligands for use in a binding assay for proteases and phosphatases, which contain cysteine in their binding sites or as a necessary structural component for enzymatic binding. The sulfhydryl group of cysteine is the nucleophilic group in the enzyme's mechanistic proteolytic and hydrolytic properties. The assay can be used to determine the ability of new, unknown ligands and mixtures of compounds to competitively bind with the enzyme versus a known binding agent for the enzyme, e.g., a known enzyme inhibitor. By the use of a mutant form of the natural or native wild-type enzyme, in which serine, or another amino acid, e.g., alanine, replaces cysteine, the problem of interference from extraneous oxidizing and alkylating agents in the assay procedure is overcome. The interference arises because of oxidation or alkylation of the sulfhydryl, —SH (or —S−), in the cysteine, which then adversely affects the binding ability of the enzyme. Specifically disclosed is an assay for tyrosine phosphatases and cysteine proteases, including caspases and cathepsins, e.g., Cathepsin K(O2), utilizing scintillation proximity assay (SPA) technology. The assay has important applications in the discovery of compounds for the treatment and study of, for example, diabetes, immunosuppression, cancer, Alzheimer's disease and osteoporosis. The novel feature of the use of a mutant enzyme can be extended to its use in a wide variety of conventional colorimetric, photometric, spectrophotometric, radioimmunoassay and ligand-binding competitive assays.
摘要翻译：公开了用于蛋白酶和磷酸酶的结合测定中的新配体，其在其结合位点含有半胱氨酸或作为酶结合的必需结构组分。半胱氨酸的巯基是酶的机理蛋白水解和水解性质中的亲核基团。该测定法可用于测定新的未知配体和化合物的混合物与酶竞争性结合的能力，与酶的已知结合剂，例如已知的酶抑制剂。通过使用天然或天然野生型酶的突变形式，其中丝氨酸或另一氨基酸例如丙氨酸取代半胱氨酸，克服了测定程序中来自外来氧化和烷化剂的干扰问题。干扰是由于半胱氨酸中巯基-SH（或-S-）的氧化或烷基化而产生的，其然后不利地影响酶的结合能力。具体公开的是利用闪烁近邻测定（SPA）技术的酪氨酸磷酸酶和半胱氨酸蛋白酶的测定法，包括胱天蛋白酶和组织蛋白酶，例如组织蛋白酶K（O 2）。该测定在发现用于治疗和研究例如糖尿病，免疫抑制，癌症，阿尔茨海默氏病和骨质疏松症的化合物中具有重要应用。使用突变酶的新颖特征可以扩展到其在各种常规比色，光度，分光光度，放射免疫测定和配体结合竞争性测定中的用途。

4. 发明授权

US06066715A Ligands for phosphatase binding assay 失效
标题翻译：用于磷酸酶结合测定的配体
公开(公告)号：US06066715A
公开(公告)日：2000-05-23
申请号：US964308
申请日：1997-11-04
申请人： Sylvie Desmarais , Richard Friesen , Robert Zamboni
发明人： Sylvie Desmarais , Richard Friesen , Robert Zamboni
IPC分类号： G01N33/566 , C07K5/08 , C12Q1/37 , C12Q1/42 , G01N33/573 , A61K38/00 , A61K38/06
CPC分类号： C07K5/0827
摘要： Disclosed are new ligands for use in a binding assay for proteases and phosphatases, which contain cysteine in their binding sites or as a necessary structural component for enzymatic binding. The sulfihydryl group of cysteine is the nucleophilic group in the enzyme's mechanistic proteolytic and hydrolytic properties. The assay can be used to determine the ability of new, unknown ligands and mixtures of compounds to competitively bind with the enzyme versus a known binding agent for the enzyme, e.g., a known enzyme inhibitor. By the use of a mutant form of the natural or native wild-type enzyme, in which serine, or another amino acid, e.g., alanine, replaces cysteine, the problem of interference from extraneous oxidizing and alkylating agents in the assay procedure is overcome. The interference arises because of oxidation or alkylation of the sulfihydryl, --SH (or --S.sup.-), in the cysteine, which then adversely affects the binding ability of the enzyme. Specifically disclosed is an assay for tyrosine phosphatases and cysteine proteases, including capsases and cathepsins, e.g., Cathepsin K(O2), utilizing scintillation proximity assay (SPA) technology. The assay has important applications in the discovery of compounds for the treatment and study of, for example, diabetes, immunosuppression, cancer, Alzheimer's disease and osteoporosis. The novel feature of the use of a mutant enzyme can be extended to its use in a wide variety of conventional colorimetric, photometric, spectrophotometric, radioimmunoassay and ligand-binding competitive assays.
摘要翻译：公开了用于蛋白酶和磷酸酶的结合测定中的新配体，其在其结合位点含有半胱氨酸或作为酶结合的必需结构组分。半胱氨酸的巯基是酶的机理蛋白水解和水解性质中的亲核基团。该测定法可用于测定新的未知配体和化合物的混合物与酶竞争性结合的能力，与酶的已知结合剂，例如已知的酶抑制剂。通过使用天然或天然野生型酶的突变形式，其中丝氨酸或另一氨基酸例如丙氨酸取代半胱氨酸，克服了测定程序中来自外来氧化和烷化剂的干扰问题。干扰是由于半胱氨酸中的巯基-SH（或-S-）的氧化或烷基化而产生的，其然后不利地影响酶的结合能力。具体公开的是利用闪烁亲近测定（SPA）技术测定酪氨酸磷酸酶和半胱氨酸蛋白酶，包括热囊酶和组织蛋白酶，例如组织蛋白酶K（O 2）。该测定在发现用于治疗和研究例如糖尿病，免疫抑制，癌症，阿尔茨海默氏病和骨质疏松症的化合物中具有重要应用。使用突变酶的新颖特征可以扩展到其在各种常规比色，光度，分光光度，放射免疫测定和配体结合竞争性测定中的用途。

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