源自过氧化物酶体增殖物激活受体γ激动剂的G蛋白偶联受体120选择性激动剂的鉴定。
Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists.
作者信息
Suzuki Takayoshi, Igari Sou-Ichi, Hirasawa Akira, Hata Mie, Ishiguro Masaji, Fujieda Hiroki, Itoh Yukihiro, Hirano Tatsuya, Nakagawa Hidehiko, Ogura Michitaka, Makishima Makoto, Tsujimoto Gozoh, Miyata Naoki
机构信息
Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
出版信息
J Med Chem. 2008 Dec 11;51(23):7640-4. doi: 10.1021/jm800970b.
A weak, nonselective G protein-coupled receptor 120 (GPR120) agonist 10 was found by screening a series of carboxylic acids derived from the peroxisome proliferator-activated receptor gamma (PPARgamma) agonist 3. Modification based on the homology model of GPR120 led to the first GPR120-selective agonist 12. These results provide a basis for constructing new tools for probing the biology of GPR120 and for developing new candidate therapeutic agents.
通过筛选一系列源自过氧化物酶体增殖物激活受体γ（PPARγ）激动剂3的羧酸，发现了一种弱的、非选择性的G蛋白偶联受体120（GPR120）激动剂10。基于GPR120的同源模型进行修饰，得到了首个GPR120选择性激动剂12。这些结果为构建用于探究GPR120生物学特性的新工具以及开发新的候选治疗药物提供了基础。
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