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1. 发明申请

WO2007027661A3 HUMAN G PROTEIN-COUPLED RECEPTOR AND MODULATORS THEREOF FOR THE TREATMENT OF ATHEROSCLEROSIS AND ATHEROSCLEROTIC DISEASE AND FOR THE TREATMENT OF CONDITIONS RELATED TO MCP-1 EXPRESSION 审中-公开
公开(公告)号：WO2007027661A3
公开(公告)日：2007-03-08
申请号：PCT/US2006/033651
申请日：2006-08-29
申请人： ARENA PHARMACEUTICALS, INC. , HAKAK, Yaron , UNETT, David J. , GATLIN, Joel , LIAW, Chen W.
发明人： HAKAK, Yaron , UNETT, David J. , GATLIN, Joel , LIAW, Chen W.
IPC分类号： G01N33/74 , C07K14/72
摘要： The present invention relates to methods of using a G protein-coupled receptor (GPCR), for example GPR84, to identify whether a candidate compound is a modulator of atherogenesis. In certain embodiments, the GPCR couples to Gi. In certain embodiments, the GPCR is human. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of atherosclerosis and atherosclerotic disease, including coronary artery disease, myocardial infarction, peripheral arterial disease, and ischemic stroke. Agonists of the invention are additionally useful as therapeutic agents for the prevention or treatment of conditions related to MCP-I expression, including but not limited to rheumatoid arthritis, Crohn's disease, and multiple sclerosis.

2. 发明申请

WO2007047520A1 GPR22 AND METHODS RELATING THERETO 审中-公开
标题翻译： GPR22及其相关方法
公开(公告)号：WO2007047520A1
公开(公告)日：2007-04-26
申请号：PCT/US2006/040226
申请日：2006-10-12
申请人： ARENA PHARMACEUTICALS, INC. , LIAW, Chen W.
发明人： LIAW, Chen W.
IPC分类号： C12N15/09
CPC分类号： C07K14/705
摘要： Methods for generating an expression-enhanced GPR22 nucleic acid, as well as substituted GPR22 nucleic acids providing for enhanced expression of the encoded GPR22 polypeptide, are provided. In practicing the subject methods, a nucleic acid encoding a mammalian GPR22 receptor polypeptide (e.g., a wild-type nucleic acid) is expression-enhanced by identifying the various codons of the coding region for the GPR22 amino acid sequence and substituting nucleotides so as to enhance expression without changing the amino acid sequence of the encoded GPR22 polypeptide. Methods, compositions, and kits using the same for screening of modulators of GPR22 are also provided.
摘要翻译：提供了产生表达增强的GPR22核酸的方法，以及提供编码的GPR22多肽的增强表达的取代的GPR22核酸。在实施本发明方法中，通过鉴定GPR22氨基酸序列的编码区的各种密码子并用核苷酸取代编码哺乳动物GPR22受体多肽（例如野生型核酸）的核酸，可以表达增强，从而增强表达而不改变编码的GPR22多肽的氨基酸序列。还提供了用于筛选GPR22调节剂的方法，组合物和试剂盒。

3. 发明申请

WO2007058930A1 HUMAN G PROTEIN-COUPLED RECEPTOR AND MODULATORS THEREOF FOR THE TREATMENT OF OBESITY AND CONDITIONS RELATED THERETO 审中-公开
标题翻译：人G蛋白相关受体及其调节剂用于治疗与之相关的肥胖和病症
公开(公告)号：WO2007058930A1
公开(公告)日：2007-05-24
申请号：PCT/US2006/043761
申请日：2006-11-08
申请人： ARENA PHARMACEUTICALS, INC. , BAGNOL, Didier , LIAW, Chen W.
发明人： BAGNOL, Didier , LIAW, Chen W.
IPC分类号： A01K67/027 , G01N33/566 , A61P3/04
CPC分类号： G01N33/74 , A01K67/0276 , A01K2217/075 , A01K2227/105 , A01K2267/0362 , A61K38/177 , A61K49/0008 , C07K14/705 , C07K14/723 , C07K2319/00 , C12N15/8509 , G01N33/53 , G01N33/566 , G01N2333/726 , G01N2500/04 , G01N2500/10 , G01N2800/044
摘要： The present invention relates to methods of using a G protein-coupled receptor (GPCR) to screen one or more candidate compounds as a modulator of body mass or of adiposity or of percentage body fat in a subject or as a pharmaceutical agent for obesity and conditions related thereto. Inverse agonists and antagonists of the invention are useful as therapeutic agents for the prevention or treatment of obesity and conditions related thereto, including hypertension, insulin resistance, metabolic syndrome, Type 2 diabetes, dyslipidemia, atherosclerosis, coronary heart disease, and stroke. Agonists and partial agonists of the invention are useful as therapeutic agents for the prevention or treatment of disorders ameliorated by increasing body mass including, but not limited to, cachexia.
摘要翻译：本发明涉及使用G蛋白偶联受体（GPCR）筛选一种或多种候选化合物作为体重或脂肪或身体脂肪在受试者体内或作为肥胖和病症的药剂的调节剂的方法相关。本发明的反向激动剂和拮抗剂可用作预防或治疗肥胖及其相关病症的治疗剂，包括高血压，胰岛素抵抗，代谢综合征，2型糖尿病，血脂异常，动脉粥样硬化，冠心病和中风。本发明的激动剂和部分激动剂可用作预防或治疗通过增加体重而改善的疾病的治疗剂，包括但不限于恶病质。

4. 发明申请

WO2007021744A1 METHODS FOR DETERMINING PROBABILITY OF AN ADVERSE OR FAVORABLE REACTION TO A NIACIN RECEPTOR AGONIST 审中-公开
标题翻译：确定不良反应对NIACIN受体激动剂的可行性的方法
公开(公告)号：WO2007021744A1
公开(公告)日：2007-02-22
申请号：PCT/US2006/031032
申请日：2006-08-09
申请人： ARENA PHARMACEUTICALS, INC. , LIAW, Chen W. , KANEMITSU-PARKS, Martha , RICHMAN, Jeremy G. , MACIEJEWSKI-LENOIR, Dominique , CONNOLLY, Daniel T.
发明人： LIAW, Chen W. , KANEMITSU-PARKS, Martha , RICHMAN, Jeremy G. , MACIEJEWSKI-LENOIR, Dominique , CONNOLLY, Daniel T.
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6883 , C12Q2600/156 , C12Q2600/158
摘要： The present invention relates generally to a GPR109A niacin receptor. The present invention relates more particularly to a method of determining an individual's probability for a condition associated with a functional niacin receptor-mediated signal response, by: (a) obtaining a GPR109A receptor nucleic acid sequence or a GPR109A receptor amino acid sequence for the individual; (b) identifying within the nucleic acid sequence or the amino acid sequence a nucleotide at a position corresponding to nucleotide position 951 of SEQ ID NO:1 or an amino acid at a position corresponding to amino acid position 317 of SEQ ID NO:2; and (c) assigning the level of probability to the individual for the condition associated with a functional niacin receptor-mediated signal response. In one embodiment, the present invention relates to assessing a GPR109A polymorphism in an individual and determining the level of probability for the subject for experiencing an adverse reaction, wherein the individual's GPR109A zygosity is predictive of the probability for a cutaneous flushing response that can be experienced following administration of a GPR109A receptor agonist.
摘要翻译：本发明一般涉及一种GPR109A烟酸受体。本发明更具体地涉及通过以下方式确定个体与功能性烟酸受体介导的信号反应相关的病症概率的方法：（a）获得个体的GPR109A受体核酸序列或GPR109A受体氨基酸序列 ; （b）在核酸序列或氨基酸序列内鉴定对应于SEQ ID NO：1的核苷酸位置951的位置处的核苷酸或对应于SEQ ID NO：2的氨基酸位置317位置的氨基酸; 和（c）为与功能性烟酸受体介导的信号反应相关的病症向个体分配概率水平。在一个实施方案中，本发明涉及评估个体中的GPR109A多态性并确定受试者经历不良反应的概率水平，其中个体的GPR109A接合度预测可以经历的皮肤潮红反应的概率之后给予GPR109A受体激动剂。

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