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Therapeutic potential of melanin-concentrating hormone-1 receptor antagonists for the treatment of obesity.

机译:黑色素浓缩激素-1受体拮抗剂治疗肥胖症的治疗潜力。

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摘要

The compelling genetic and pharmacological evidence implicating melanin-concentrating hormone-1 receptor (MCH-1R) signalling in the regulation of food intake and energy expenditure has generated a great deal of interest by pharmaceutical companies for the discovery of MCH-1R antagonists, evidenced by the increased number of patents describing MCH-1R antagonists for the treatment of obesity and metabolic syndrome. The structural diversity of small molecular weight drug-like MCH-1R antagonists produced and preclinical studies showing hypophagia and weight loss with small molecular weight and peptidal antagonists in rodents is encouraging and suggests that the identification of clinical candidates will be forthcoming.
机译:有说服力的遗传和药理学证据牵涉黑色素浓缩激素1受体(MCH-1R)信号调节食物摄入和能量消耗,这引起了制药公司对发现MCH-1R拮抗剂的浓厚兴趣,这一点得到了证明。描述用于治疗肥胖症和代谢综合征的MCH-1R拮抗剂的专利数量增加。产生的小分子药物样MCH-1R拮抗剂的结构多样性和临床前研究表明,啮齿类动物的小分子和肽类拮抗剂存在吞噬和体重减轻,这令人鼓舞,并表明即将进行临床候选者的鉴定。

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