Ago-allosteric modulators of human glucagon-like peptide 2 receptor |
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Authors: | Kazuto Yamazaki Hiroki Terauchi Daisuke Iida Hironori Fukumoto Shuichi Suzuki Takaki Kagaya Mika Aoki Koichiro Koyama Takashi Seiki Kazuma Takase Misako Watanabe Tohru Arai Kappei Tsukahara Junichi Nagakawa |
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Affiliation: | Eisai Product Creation Systems, Eisai Co., Ltd., 5-1-3 Tokodai, Tsukuba, Ibaraki 300-2635, Japan. Electronic address: k5-yamazaki@hhc.eisai.co.jp. |
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Abstract: | ![]() Glucagon-like peptide 2 (GLP-2) is an intestinotropic peptide that binds to GLP-2 receptor (GLP-2R), a class-B G protein-coupled receptor (GPCR). Few synthetic agonists have been reported so far for class-B GPCRs. Here, we report the first scaffold compounds of ago-allosteric modulators for human GLP-2R, derived from methyl 2-{[(2Z)-2-(2,5-dichlorothiophen-3-yl)-2-(hydroxyimino)ethyl]sulfanyl}benzoate (compound 1). |
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