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Ago-allosteric modulators of human glucagon-like peptide 2 receptor
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
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.
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).
Keywords:
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