Identification of G protein-coupled receptor 120-selective agonists derived from PPARγ agonists

被引：94

作者：

Suzuki, Takayoshi ^{[2
]}

Igari, Sou-Ichi ^{[2
]}

Hirasawa, Akira ^{[1
]}

Hata, Mie ^{[3
]}

Ishiguro, Masaji ^{[4
,5
]}

Fujieda, Hiroki ^{[2
]}

Itoh, Yukihiro ^{[2
]}

Hirano, Tatsuya ^{[2
]}

Nakagawa, Hidehiko ^{[2
]}

Ogura, Michitaka ^{[4
,5
]}

Makishima, Makoto ^{[4
,5
]}

Tsujimoto, Gozoh ^{[1
]}

Miyata, Naoki ^{[2
]}

机构：

[1] Kyoto Univ, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 6068501, Japan

[2] Nagoya City Univ, Grad Sch Pharmaceut Sci, Mizuho Ku, Aichi 4678603, Japan

[3] JST Innovat Plaza Kyoto, Nishikyo Ku, Kyoto 6158245, Japan

[4] Niigata Univ Pharm & Appl Life Sci, Fac Pharmaceut Sci, Akiha Ku, Niigata, Japan

[5] Nihon Univ, Sch Med, Itabashi Ku, Tokyo 1738610, Japan

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 23期

关键词：

D O I：

10.1021/jm800970b

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 (PPAR gamma) 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.

引用

页码：7640 / 7644

页数：5

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