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1. 发明授权

US5837809A Mammalian opioid receptor ligand and uses 失效
标题翻译：哺乳动物阿片受体配体及用途
公开(公告)号：US5837809A
公开(公告)日：1998-11-17
申请号：US514451
申请日：1995-08-11
申请人： David K. Grandy , James R. Bunzow , Olivier Civelli , Rainer Klaus Reinscheid , Hans-Peter Nothacker , Frederick James Monsma
发明人： David K. Grandy , James R. Bunzow , Olivier Civelli , Rainer Klaus Reinscheid , Hans-Peter Nothacker , Frederick James Monsma
IPC分类号： A61K38/00 , C07K14/665 , C07K7/08 , C07K14/705
CPC分类号： C07K14/665 , A61K38/00
摘要： The present invention relates to a novel mammalian opioid receptor protein and ligands that bind to such proteins. The invention is directed toward the isolation, characterization and pharmacological use of an endogenous ligand that specifically binds to a novel mammalian opioid receptor protein heterologously expressed in mammalian cells. The invention specifically provides the isolated peptide ligand and analogues, derivatives and variants thereof. The invention specifically provides tyrosine substitution variants of the peptide ligand that specifically bind to the opioid receptor and can be radioiodinated. Also provided are methods of making such peptide ligands and methods of using the ligands for diagnostic and therapeutic uses and for the identification of other naturally-occurring or synthetic opioid receptor ligands.
摘要翻译：本发明涉及新型的哺乳动物阿片受体蛋白质和与这些蛋白质结合的配体。本发明涉及特异性结合在哺乳动物细胞中异源表达的新型哺乳动物阿片受体蛋白的内源性配体的分离，表征和药理学应用。本发明特别提供了分离的肽配体及其类似物，衍生物和变体。本发明具体提供肽配体的酪氨酸取代变体，其特异性结合阿片受体并可以放射性碘化。还提供了制备这种肽配体的方法和使用配体用于诊断和治疗用途以及鉴定其它天然存在或合成的阿片受体配体的方法。

2. 发明授权

US06406866B1 Method of screening of a compound for binding to MSOR 失效
标题翻译：筛选化合物结合MSOR的方法
公开(公告)号：US06406866B1
公开(公告)日：2002-06-18
申请号：US09048916
申请日：1998-03-26
申请人： David K. Grandy , James R. Bunzow , Olivier Civelli , Rainer Klaus Reinscheid , Hans-Peter Nothacker , Frederick James Monsma
发明人： David K. Grandy , James R. Bunzow , Olivier Civelli , Rainer Klaus Reinscheid , Hans-Peter Nothacker , Frederick James Monsma
IPC分类号： G01N3353
CPC分类号： C07K14/665 , A61K38/00 , A61K39/00 , C07K14/705 , C07K2319/00 , C12N2799/023
摘要： The present invention relates to a novel mammalian opioid receptor protein and ligands that bind to such proteins. The invention is directed toward the isolation, characterization and pharmacological use of an endogenous ligand that specifically binds to a novel mammalian opioid receptor protein heterologously expressed in mammalian cells. The invention specifically provides the isolated peptide ligand and analogues, derivatives and variants thereof. The invention specifically provides tyrosine substitution variants of the peptide ligand that specifically bind to the opioid receptor and can be radioiodinated. Also provided are methods of making such peptide ligands and methods of using the ligands for diagnostic and therapeutic uses and for the identification of other naturally-occurring or synthetic opioid receptor ligands.
摘要翻译：本发明涉及新型的哺乳动物阿片受体蛋白质和与这些蛋白质结合的配体。本发明涉及特异性结合在哺乳动物细胞中异源表达的新型哺乳动物阿片受体蛋白的内源性配体的分离，表征和药理学应用。本发明特别提供了分离的肽配体及其类似物，衍生物和变体。本发明具体提供肽配体的酪氨酸取代变体，其特异性结合阿片受体并可以放射性碘化。还提供了制备这种肽配体的方法和使用配体用于诊断和治疗用途以及鉴定其它天然存在或合成的阿片受体配体的方法。

3. 发明授权

US06790608B2 Methods of identifying and ADP-glucose receptor ligand, agonist or antagonist 有权
标题翻译：识别ADP-葡萄糖受体配体，激动剂或拮抗剂的方法
公开(公告)号：US06790608B2
公开(公告)日：2004-09-14
申请号：US09780576
申请日：2001-02-09
申请人： Olivier Civelli , Hans-Peter Nothacker , Zhiwei Wang , Rainer Reinscheid
发明人： Olivier Civelli , Hans-Peter Nothacker , Zhiwei Wang , Rainer Reinscheid
IPC分类号： C12Q100
CPC分类号： G01N33/66
摘要： The present invention provides an isolated nucleic acid molecule containing a nucleotide sequence which encodes an ADP-glucose receptor, and isolated polynucleotides therefrom. Also provided is an isolated ADP-glucose receptor polypeptide, an isolated immunogenic peptide therefrom, and antibodies specific therefor. The invention also provides a method of identifying an ADP-glucose receptor agonist or antagonist, by contacting an ADP-glucose receptor with one or more candidate compounds under conditions suitable for detection of a G-protein coupled signal in response to ADP-glucose, and identifying a candidate compound that alters production of the signal. Further provided is a method of identifying an ADP-glucose receptor ligand, by contacting an ADP-glucose receptor with one or more candidate compounds under conditions suitable for detecting selective binding of ADP-glucose to ADP-glucose receptor, and identifying a candidate compound that selectively binds the ADP-glucose receptor. Also provided are methods of diagnosing or determining susceptibility to ADP-glucose receptor associated conditions, by detecting in a sample from the individual expression of ADP glucose receptor nucleic acid molecules or polypeptides.
摘要翻译：本发明提供了分离的核酸分子，其含有编码ADP-葡萄糖受体的核苷酸序列及其分离的多核苷酸。还提供了分离的ADP-葡萄糖受体多肽，其中分离的免疫原性肽及其特异性抗体。本发明还提供了通过在适于检测响应于ADP-葡萄糖的G蛋白偶联信号的条件下使ADP-葡萄糖受体与一种或多种候选化合物接触来鉴定ADP-葡萄糖受体激动剂或拮抗剂的方法，以及识别改变信号产生的候选化合物。进一步提供的是通过在适于检测ADP-葡萄糖与ADP-葡萄糖受体的选择性结合的条件下将ADP-葡萄糖受体与一种或多种候选化合物接触并鉴定候选化合物来鉴定ADP-葡萄糖受体配体的方法选择性结合ADP-葡萄糖受体。还提供了通过在来自ADP葡萄糖受体核酸分子或多肽的个体表达的样品中检测来诊断或确定对ADP-葡萄糖受体相关病症易感性的方法。

4. 发明授权

US06326156B1 Method of identifying compounds having antiepileptic anticonvulsant or anxiolytic activities 失效
标题翻译：鉴定具有抗癫痫抗惊厥或抗焦虑活性的化合物的方法
公开(公告)号：US06326156B1
公开(公告)日：2001-12-04
申请号：US08868355
申请日：1997-06-03
申请人： Olivier Civelli , James Richard Martin , Frederick Monsma , Jean-Luc Moreau , Hans-Peter Nothacker , Rainer Reinscheid
发明人： Olivier Civelli , James Richard Martin , Frederick Monsma , Jean-Luc Moreau , Hans-Peter Nothacker , Rainer Reinscheid
IPC分类号： G01N3353
CPC分类号： G01N33/9486 , G01N33/566 , G01N2500/00
摘要： The present invention relates to a method of screening for a therapeutically useful compound which comprises testing an LC132 receptor agonist in a screening assay for psychiatric and/or neurological disorders. More particularly, the screening method is based on contacting an LC132 receptor with an agent suspected of being an agonist of the LC132 receptor function, followed by the detection of the binding and/or the agonist activity of the compound and then testing of an agent with LC132 agonist activity in an antiepileptic, anticonvulsant or anxiolytic screening assay.
摘要翻译：本发明涉及一种筛选治疗有用化合物的方法，其包括在精神和/或神经障碍的筛选测定中检测LC132受体激动剂。更具体地，筛选方法是基于将LC132受体与疑似是LC132受体功能的激动剂的试剂接触，然后检测化合物的结合和/或激动剂活性，然后测试具有抗癫痫药，抗惊厥药或抗焦虑药物筛选试验中LC132激动剂活性。

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