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2. 发明申请

US20160130322A1 A GROWTH HORMONE SECRETAGOGUE RECEPTOR BASED PROTEIN, NUCLEIC ACIDS AND METHODS AND USES THEREOF 有权
标题翻译：一种生长激素基质蛋白受体基因蛋白，核酸及其方法及用途
公开(公告)号：US20160130322A1
公开(公告)日：2016-05-12
申请号：US14776318
申请日：2014-03-14
申请人： Qinghua Wang
发明人： Qinghua Wang , Younes Anini
IPC分类号： C07K14/72 , A61K48/00
CPC分类号： C07K14/723 , A61K48/00 , C07K14/72 , C07K2319/30 , C07K2319/32
摘要： Ghrelin is a peptide hormone that binds its receptor, growth hormone secretatgogue receptor 1a (GHS-R1 a, ghrelin receptor), to promote adiposity and obesity in mammals. Ghrelin and its receptor are targets for therapeutic intervention to treat obesity-related disease and cancer. A soluble decoy GHS-R1 a receptor is developed that binds ghrelin in the periphery, preventing ghrelin from binding GHS-R1 on cells, thereby antagonizing ghrelin to treat obesity-related pathological conditions and cancer. GHS-R1 a is a transmembrane protein comprising an N-terminal extracellular domain (Nt), seven transmembrane regions and three extracellular loops (EC1, EC2 and EC3). The Nt, EC1 and EC2 are linked together, in the absence of the transmembrane regions, and fused to a Fc from an immunoglobulin, to create the decoy GHS-R1 a fusion protein, GHSR-Fc. The GHSR-Fc inhibits adiposity and weight gain in mice on a high fat diet (HFD), while the Nt and ECs on their own have no significant effect.
摘要翻译：生长素释放肽是一种能与其受体，生长激素分泌受体1a（GHS-R1a，生长素释放肽受体）结合的肽激素，以促进哺乳动物的肥胖和肥胖。生长素释放肽及其受体是用于治疗肥胖相关疾病和癌症的治疗干预的目标。开发了可溶性诱饵GHS-R1 a受体，其结合周围的生长素释放肽，阻止生长素释放肽与细胞结合GHS-R1，从而拮抗生长素释放肽来治疗肥胖相关的病理状况和癌症。 GHS-R1a是包含N-末端胞外结构域（Nt），七个跨膜区和三个胞外环（EC1，EC2和EC3）的跨膜蛋白。 Nt，EC1和EC2在不存在跨膜区的情况下连接在一起，并与来自免疫球蛋白的Fc融合，以产生诱饵GHS-R1融合蛋白GHSR-Fc。 GHSR-Fc在高脂肪饮食（HFD）中抑制小鼠的肥胖和体重增加，而Nt和ECs本身没有显着影响。

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