首个用于GPR120（FFA4）成像的环境敏感型荧光探针的发现。
Discovery of the First Environment-Sensitive Fluorescent Probe for GPR120 (FFA4) Imaging.
作者信息
Liu Jiaxiang, Tian Chengsen, Jiang Tianyu, Gao Yuqi, Zhou Yubin, Li Minyong, Du Lupei
机构信息
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan, Shandong 250012, China.
School of Chemical Engineering, Qilu Normal University, Jinan, Shandong 250200, China.
出版信息
ACS Med Chem Lett. 2017 Mar 27;8(4):428-432. doi: 10.1021/acsmedchemlett.7b00023. eCollection 2017 Apr 13.
GPR120, which is activated by long-chain free fatty acids (FFAs), has been recognized as a new attractive target for the treatment of type 2 diabetes and metabolic disease. The visualization and location of GPR120 in native cells can provide powerful information for guiding the physiological and pathological studies of GPR120. We report herein the first potent fluorescent probes that sensitively detect GPR120. We designed and synthesized a series of novel environment-sensitive probes with suitable fluorescence property, high biological activity on the GPR120, and acceptable cytotoxicity. These fluorescent probes targeting GPR120 are expected to expand the toolkit for further studies on GPR120.
GPR120由长链游离脂肪酸（FFA）激活，已被公认为是治疗2型糖尿病和代谢性疾病的一个新的有吸引力的靶点。GPR120在天然细胞中的可视化和定位可为指导GPR120的生理和病理研究提供有力信息。我们在此报告了首个能灵敏检测GPR120的强效荧光探针。我们设计并合成了一系列具有合适荧光特性、对GPR120具有高生物活性且细胞毒性可接受的新型环境敏感探针。这些靶向GPR120的荧光探针有望扩展用于进一步研究GPR120的工具集。
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