参与代谢疾病的GPCRs:药物治疗发展更新
Cheng Jin1,2, Hui Chen1, Li Xie1
1Department of Medical Microbiology & Parasitology, MOE/NHC/CAMS Key Laboratory of Medical Molecular Virology, School of Basic Medical Sciences, Fudan University Shanghai Medical College, Shanghai, 200032, China.
G蛋白结合受体 (GPCRs) 调节了新陈代谢的平衡. 新型GPCR激活剂和对抗剂在治疗糖尿病和脂质失调等代谢疾病方面表现有前途.
科学领域:
- 代谢研究的研究.
- 药理学 药理学是指药理学的学科.
- 内分泌学 在内分泌学.
背景情况:
- G蛋白结合受体 (GPCR) 在代谢途径中至关重要,影响营养处理和胰岛素敏感性.
- GPCRs的调节失调与全球代谢障碍的患病率上升有关.
- 审查的关键GPCRs包括GPR91,GPR55,GPR119,GPR109a,GPR142,GPR40,GPR41,GPR43和GPR120.这些GPCRs的基因组分别是:
研究的目的:
- 审查GPCR对代谢恒温的调节.
- 探索特定GPCRs在主要代谢疾病中的作用.
- 总结针对GPCRs治疗开发的药理学候选药物.
主要方法:
- 对GPCR结构,信号和代谢中的功能进行文献综述.
- 针对已审查的GPCRs的小分子激动剂和对抗剂的汇编.
- 对GPCR向治疗药物的临床前和临床试验数据的分析.
主要成果:
- GPCRs显著影响营养合成,运输,储存和胰岛素敏感性.
- GPCRs与代谢综合征,糖尿病,失脂症和非酒精性脂肪肝炎有关.
- 已经确定了许多小分子激动剂和对抗剂,具有有希望的临床前和临床数据.
结论:
- GPCRs代表了代谢疾病干预的关键目标.
- 调节GPCR的药物有可能成为新药治疗代谢障碍的新药.
- 对GPCR机制和药物开发的进一步研究是有必要的.
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