首页> 外国专利> GPR101 receptor in a method for identifying modulators of hypothalamic proopiomelanocortin (POMC) -derived bioactive peptide secretion useful in the treatment of disorders associated with hypothalamic proopiomelanocortin (POMC) derived bioactive peptides Use of

GPR101 receptor in a method for identifying modulators of hypothalamic proopiomelanocortin (POMC) -derived bioactive peptide secretion useful in the treatment of disorders associated with hypothalamic proopiomelanocortin (POMC) derived bioactive peptides Use of

机译：GPR101受体，用于鉴定下丘脑原黑素皮质激素（POMC）衍生的生物活性肽分泌调节剂的方法，可用于治疗与下丘脑原黑素皮质激素（POMC）衍生的生物活性肽相关的疾病

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摘要

The present invention relates to methods of using GPR101 G protein-coupled receptor (GPCR) to screen candidate compounds as modulators of hypothalamic proopiomelanocortin (POMC)-derived biologically active peptide secretion. Modulators of GPR101 receptor modulate hypothalamic POMC-derived biologically active peptide secretion and are useful in the treatment of POMC-derived biologically active peptide-related disorders. POMC-derived biologically active peptides include, but are not limited to, -melanocyte stimulating hormone (-MSH), -melanocyte stimulating hormone (-MSH) and -melanocyte stimulating hormone (-MSH). Agonists and partial agonists of GPR101 receptor stimulate hypothalamic -MSH, -MSH and -MSH secretion and are useful, for example, in the treatment and prevention of obesity and conditions related thereto (including but not limited to Type 2 diabetes, insulin resistance, and metabolic syndrome), inflammation-associated disorders, and pyrexia. Inverse agonists and antagonists of GPR101 receptor inhibit -MSH, -MSH and -MSH secretion and are useful, for example, in the treatment and prevention of disorders such as cachexia.

机译：本发明涉及使用GPR101G蛋白偶联受体（GPCR）来筛选候选化合物作为下丘脑的原皮黑素皮质激素（POMC）衍生的生物活性肽分泌的调节剂的方法。 GPR101受体的调节剂调节下丘脑POMC衍生的生物活性肽的分泌，可用于治疗POMC衍生的生物活性肽相关的疾病。源自POMC的生物活性肽包括但不限于，-黑素细胞刺激激素（-MSH），-黑素细胞刺激激素（-MSH）和-黑素细胞刺激激素（-MSH）。 GPR101受体的激动剂和部分激动剂可刺激下丘脑-MSH，-MSH和-MSH分泌，例如可用于治疗和预防肥胖症及其相关病症（包括但不限于2型糖尿病，胰岛素抵抗和代谢综合征），炎症相关疾病和发热。 GPR101受体的反向激动剂和拮抗剂可抑制-MSH，-MSH和-MSH分泌，例如可用于治疗和预防疾病，例如恶病质。

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公开/公告号JP2009538623A

专利类型
公开/公告日2009-11-12

原文格式PDF
申请/专利权人アリーナファーマシューティカルズ;インコーポレイテッド;
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申请/专利号JP20090513258
发明设计人バニョル;ディディエ;
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申请日2007-05-30
分类号C12Q1/02;C12N15/09;G01N33/50;G01N33/15;C07K14/705;
国家 JP
入库时间 2022-08-21 19:01:11

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