摘要
血管紧张素Ⅱ 2型受体(angiotensin receptor type 2, AT2R)是血管紧张素Ⅱ (angiotensin Ⅱ, Ang Ⅱ)受体亚型之一,选择性激动或拮抗AT2受体可引起血管舒张、抗细胞增殖、促突起生长、阻断神经元兴奋性等。AT2受体可作为潜在的药物靶标用于心血管疾病、纤维化、炎症、神经元疾病和肿瘤等疾病的治疗。新型选择性作用于AT2受体的药物研发以及AT2受体参与的细胞内信号转导机制的研究是一个具有挑战性但值得深入研究的领域。本文对AT2受体蛋白的研究进展以及作用于AT2受体化合物的研究进行阐述,结合构效关系分析,为该领域进一步的研究提供借鉴和指导。
Selective activation or inhibition of the angiotensin Ⅱ type 2(AT2) receptor can cause vasodilation,decrease cell proliferation, promote neurite outgrowth and block neuronal excitability. The AT2 receptor can be used as a potential drug target for the treatment of cardiovascular diseases, fibrosis, inflammation, neuronal diseases and tumors. Research and development of new drugs that selectively act on the AT2 receptor and the mechanism of intracellular signal transduction involving the AT2 receptor is a challenging but worthy endeavor. We review research progress on the AT2 receptor and compounds that act on the AT2 receptor, along with structure-activity relationship analysis, to provide reference and guidance for further research in this field.
作者
张艳春
张祖志
徐进宜
王丹慧
徐梅月
ZHANG Yan-chun;ZHANG Zu-zhi;XU Jin-yi;WANG Dan-hui;XU Mei-yue(College of Pharmacy,Anhui University of Chinese Medicine,Hefei 230012,China;Anhui Province Key Laboratory of Chinese Medicinal Formula,Hefei 230012,China;School of Pharmacy,China Pharmaceutical University,Nanjing 210009,China)
出处
《药学学报》
CAS
CSCD
北大核心
2021年第3期711-722,共12页
Acta Pharmaceutica Sinica
基金
安徽省自然科学基金面上项目(1908085MH269)。
关键词
血管紧张素Ⅱ2型受体
激动剂
拮抗剂
选择性
构效关系
angiotensin receptor type 2 receptor
agonist
antagonist
selectivity
structure and activity relationship