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1. 发明授权

US5846819A Recombinant expression vectors for expression of heterologous proteins 失效
标题翻译：用于表达异源蛋白质的重组表达载体
公开(公告)号：US5846819A
公开(公告)日：1998-12-08
申请号：US472045
申请日：1995-06-06
申请人： Mark H. Pausch , Bradley A. Ozenberger , John R. Hadcock , Laura A. Price , Eileen M. Kajkowski , Donald R. Kirsch , Deborah T. Chaleff
发明人： Mark H. Pausch , Bradley A. Ozenberger , John R. Hadcock , Laura A. Price , Eileen M. Kajkowski , Donald R. Kirsch , Deborah T. Chaleff
IPC分类号： C12N15/09 , C07K14/72 , C12N1/15 , C12N1/19 , C12N15/12 , C12P21/02 , C12Q1/02 , C12R1/865 , C12N15/63 , C07K14/705
CPC分类号： C07K14/723 , C07K2319/00
摘要： The present invention is directed to a expression vectors and yeast cells transformed therewith containing a first heterologous nucleotide sequence which codes for a G protein-coupled receptor, for example, the somatostatin receptor, and a second nucleotide sequence which codes for all or a portion of a G protein .alpha..beta..gamma. complex. Said heterologous protein is physically expressed in a host cell membrane in proper orientation for both stereoselective binding of ligands, as well as functional interaction with G proteins on the cytoplasmic side of the cell membrane. In some embodiments, a nucleotide sequence encoding a heterologous or chimeric G.alpha. protein is expressed in conjunction with nucleotide sequences from the yeast G protein .beta..gamma. subunits. A second aspect of the present invention provides expression vectors and transformed yeast cells encoding chimeric yeast/heterologous G protein coupled receptors. A third aspect of the present invention is directed to methods of assaying compounds using these expression constructs and yeast cell expression systems to determine the effects of ligand binding to the heterologous receptors expressed in the systems.
摘要翻译：本发明涉及转化的表达载体和酵母细胞，其含有编码G蛋白偶联受体（例如生长抑素受体）的第一异源核苷酸序列，以及编码全部或一部分的第二核苷酸序列一个G蛋白αβγ复合物。所述异源蛋白质在适当取向的宿主细胞膜中物理表达，用于配体的立体选择性结合，以及与细胞膜细胞质侧上的G蛋白的功能相互作用。在一些实施方案中，编码异源或嵌合Gα蛋白的核苷酸序列与来自酵母G蛋白βγ亚基的核苷酸序列一起表达。本发明的第二方面提供了编码嵌合酵母/异源G蛋白偶联受体的表达载体和转化的酵母细胞。本发明的第三方面涉及使用这些表达构建体和酵母细胞表达系统测定化合物以确定配体与系统中表达的异源受体结合的作用的方法。

2. 发明授权

US6162455A Method for increasing lean meat, improving the lean meat to fat ratio and improving amino acid utilization in warm-blooded animals 失效
标题翻译：增加瘦肉，提高瘦肉比，提高温血动物氨基酸利用率的方法
公开(公告)号：US6162455A
公开(公告)日：2000-12-19
申请号：US986522
申请日：1997-12-08
申请人： Ralph M. Cleale, IV , Mark H. Pausch , John R. Hadcock
发明人： Ralph M. Cleale, IV , Mark H. Pausch , John R. Hadcock
IPC分类号： A23K1/16 , A23K1/165
CPC分类号： A23K20/137
摘要： There is provided a method for increasing lean meat, improving the lean meat to fat ratio and improving amino acid utilization in warm-blooded animals by administering an effective amount of an alpha-2 adrenergic receptor antagonist.
摘要翻译：提供了一种通过施用有效量的α-2肾上腺素能受体拮抗剂来增加瘦肉，提高瘦肉与脂肪比并提高温血动物氨基酸利用率的方法。

3. 发明授权

US06451783B1 Treatments for obesity and methods for identifying compounds useful for treating obesity 失效
标题翻译：用于肥胖症的治疗方法和用于鉴定可用于治疗肥胖症的化合物的方法
公开(公告)号：US06451783B1
公开(公告)日：2002-09-17
申请号：US09761320
申请日：2001-01-16
申请人： John R. Hadcock , Andrew G. Swick
发明人： John R. Hadcock , Andrew G. Swick
IPC分类号： A61K3133
CPC分类号： G01N33/74 , A46B9/02 , A46B2200/3006 , A61K31/00 , A61K31/34 , A61K45/06 , G01N33/566 , G01N2333/726 , G01N2500/00
摘要： The present invention provides a method of treating obesity, sexual dysfunction (including erectile dysfunction), diabetes, insulin resistance, hyperinsulinemia, Syndrome X, adrenal dysfunction, hypertension, hypercholesterolemia, atherosclerosis, hyperlipoproteinemia, hypertriglyceridemia, or substance abuse, the method comprising the step of administering to a patent having or at risk of having one of the above-mentioned diseases a therapeutically effective amount of a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not attenuate the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors. The present invention also provides a method of identifying a compound that is useful for the treatment or prevention of obesity, sexual dysfunction (including erectile dysfunction), diabetes, insulin resistance, hyperinsulinemia, Syndrome X, adrenal dysfunction, hypertension, hypercholesterolemia, atherosclerosis, hyperlipoproteinemia, hypertriglyceridemia, or substance abuse, the method comprising the steps of: 1) determining if a compound affects the binding of agouti-related protein to melanocortin receptors; 2) determining if a compound affects the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors; and 3) selecting a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not affect the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors.
摘要翻译：本发明提供了一种治疗肥胖症，性功能障碍（包括勃起功能障碍），糖尿病，胰岛素抵抗，高胰岛素血症，综合征X，肾上腺功能障碍，高血压，高胆固醇血症，动脉粥样硬化，高脂蛋白血症，高甘油三酯血症或药物滥用的方法，对具有或具有上述疾病之一的风险的专利施用治疗有效量的化合物，其减弱agouti相关蛋白与黑皮质素受体的结合，但不会减弱α-黑素细胞刺激激素的结合到黑皮质素受体。本发明还提供了鉴定可用于治疗或预防肥胖，性功能障碍（包括勃起功能障碍），糖尿病，胰岛素抵抗，高胰岛素血症，综合征X，肾上腺功能障碍，高血压，高胆固醇血症，动脉粥样硬化，高脂蛋白血症，高甘油三酯血症或药物滥用，所述方法包括以下步骤：1）确定化合物是否影响结合蛋白与黑皮质素受体的结合; 2）确定化合物是否影响α-黑素细胞刺激激素与黑皮质素受体的结合; 和3）选择减弱agouti相关蛋白与黑皮质素受体结合的化合物，但不影响α-黑素细胞刺激激素与黑皮质素受体的结合。

4. 发明授权

US06734175B2 Treatments for obesity and methods for identifiying compounds useful for treating obesity 失效
标题翻译：用于肥胖症的治疗方法以及鉴定用于治疗肥胖症的化合物的方法
公开(公告)号：US06734175B2
公开(公告)日：2004-05-11
申请号：US10205304
申请日：2002-07-24
申请人： John R. Hadcock , Andrew G. Swick
发明人： John R. Hadcock , Andrew G. Swick
IPC分类号： A61K3133
CPC分类号： G01N33/74 , A46B9/02 , A46B2200/3006 , A61K31/00 , A61K31/34 , A61K45/06 , G01N33/566 , G01N2333/726 , G01N2500/00
摘要： The present invention provides a method of treating obesity, sexual dysfunction (including erectile dysfunction), diabetes, insulin resistance, hyperinsulinemia, Syndrome X, adrenal dysfunction, hypertension, hypercholesterolemia, atherosclerosis, hyperlipoproteinemia, hypertriglyceridemia, or substance abuse, the method comprising the step of administering to a patent having or at risk of having one of the above-mentioned diseases a therapeutically effective amount of a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not attenuate the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors. The present invention also provides a method of identifying a compound that is useful for the treatment or prevention of obesity, sexual dysfunction (including erectile dysfunction), diabetes, insulin resistance, hyperinsulinemia, Syndrome X, adrenal dysfunction, hypertension, hypercholesterolemia, atherosclerosis, hyperlipoproteinemia, hypertriglyceridemia, or substance abuse, the method comprising the steps of: 1) determining if a compound affects the binding of agouti-related protein to melanocortin receptors; 2) determining if a compound affects the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors; and 3) selecting a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not affect the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors.
摘要翻译：本发明提供了一种治疗肥胖症，性功能障碍（包括勃起功能障碍），糖尿病，胰岛素抵抗，高胰岛素血症，综合征X，肾上腺功能障碍，高血压，高胆固醇血症，动脉粥样硬化，高脂蛋白血症，高甘油三酯血症或药物滥用的方法，对具有或具有上述疾病之一的风险的专利施用治疗有效量的化合物，其减弱agouti相关蛋白与黑皮质素受体的结合，但不会减弱α-黑素细胞刺激激素的结合到黑皮质素受体。本发明还提供了鉴定可用于治疗或预防肥胖，性功能障碍（包括勃起功能障碍），糖尿病，胰岛素抵抗，高胰岛素血症，综合征X，肾上腺功能障碍，高血压，高胆固醇血症，动脉粥样硬化，高脂蛋白血症，高甘油三酯血症或药物滥用，所述方法包括以下步骤：1）确定化合物是否影响结合蛋白与黑皮质素受体的结合; 2）确定化合物是否影响α-黑素细胞刺激激素与黑皮质素受体的结合; 和3）选择减弱agouti相关蛋白与黑皮质素受体结合的化合物，但不影响α-黑素细胞刺激激素与黑皮质素受体的结合。

5. 发明授权

US06699832B2 Methods of treating obesity using a neurotensin receptor ligand 失效
标题翻译：使用神经降压素受体配体治疗肥胖症的方法
公开(公告)号：US06699832B2
公开(公告)日：2004-03-02
申请号：US09841276
申请日：2001-04-24
申请人： John R. Hadcock
发明人： John R. Hadcock
IPC分类号： A61K3100
CPC分类号： A61K45/06 , A61K31/505 , A61K38/10 , A61K2300/00
摘要： The present invention relates to methods of treating obesity, diabetes, sexual dysfunction, atherosclerosis, insulin resistance, impaired glucose tolerance, hypercholesterolemia or hypertrigylceridemia using a neurotensin receptor ligand. The present invention also relates to pharmaceutical compositions and kits that comprise a neurotensin receptor ligand.
摘要翻译：本发明涉及使用神经降压素受体配体治疗肥胖症，糖尿病，性功能障碍，动脉粥样硬化，胰岛素抵抗，葡萄糖耐量降低，高胆固醇血症或高胰岛素血症的方法。本发明还涉及包含神经降压素受体配体的药物组合物和试剂盒。

6. 发明授权

US06420137B1 Nucleic acid encoding human neurotensin subtype 2 receptor 失效
标题翻译：编码人类神经丝氨酸亚型2受体的核酸
公开(公告)号：US06420137B1
公开(公告)日：2002-07-16
申请号：US09200090
申请日：1998-11-25
申请人： Joann Strnad , John R. Hadcock
发明人： Joann Strnad , John R. Hadcock
IPC分类号： C12N1512
CPC分类号： C07K14/723 , A61K48/00
摘要： Nucleic acids encoding the long form and shorter isoform of the neurotensin receptor subtype 2, referred to as HNT2R (long) and HNT2R (short), are described. Polypeptides having amino acid sequences of the HNT2R and HNT2RS isolated proteins are also provided. A method is also provided for isolating and cloning receptors expressed from the novel HNT2R and HNT2R cDNAs for use in development/implementation of high throughput screens to identify novel neurotensin agonists and antagonists. Methods are also provided for identifying compounds that bind to HNT2R.
摘要翻译：描述了编码神经降压素受体亚型2的长形式和较短同种型的核酸，称为HNT2R（长）和HNT2R（短）。还提供了具有HNT2R和HNT2RS分离的蛋白质的氨基酸序列的多肽。还提供了用于分离和克隆由新型HNT2R和HNT2R cDNA表达的受体的方法，用于开发/实施高通量筛选以鉴定新的神经降压素激动剂和拮抗剂。还提供了用于鉴定结合HNT2R的化合物的方法。

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