title: Ago-allosteric modulators of human glucagon-like peptide 2 receptor.
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).
authors.affiliation: Eisai Product Creation Systems, Eisai Co., Ltd., 5-1-3 Tokodai, Tsukuba, Ibaraki 300-2635, Japan. k5-yamazaki@hhc.eisai.co.jp
authors.forename: Kazuto
authors.initials: K
authors.lastname: Yamazaki
authors.forename: Hiroki
authors.initials: H
authors.lastname: Terauchi
authors.forename: Daisuke
authors.initials: D
authors.lastname: Iida
authors.forename: Hironori
authors.initials: H
authors.lastname: Fukumoto
authors.forename: Shuichi
authors.initials: S
authors.lastname: Suzuki
authors.forename: Takaki
authors.initials: T
authors.lastname: Kagaya
authors.forename: Mika
authors.initials: M
authors.lastname: Aoki
authors.forename: Koichiro
authors.initials: K
authors.lastname: Koyama
authors.forename: Takashi
authors.initials: T
authors.lastname: Seiki
authors.forename: Kazuma
authors.initials: K
authors.lastname: Takase
authors.forename: Misako
authors.initials: M
authors.lastname: Watanabe
authors.forename: Tohru
authors.initials: T
authors.lastname: Arai
authors.forename: Kappei
authors.initials: K
authors.lastname: Tsukahara
authors.forename: Junichi
authors.initials: J
authors.lastname: Nagakawa
mesh_terms: D001565:Benzoates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D000067758:Glucagon-Like Peptide-2 Receptor; D006801:Humans; D015394:Molecular Structure; D018027:Receptors, Glucagon / Q000819:agonists*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D001565:Benzoates; D000067758:Glucagon-Like Peptide-2 Receptor; D018027:Receptors, Glucagon; D013876:Thiophenes; C577886:methyl 2-(((2Z)-2-(2,5-dichlorothiophen-3-yl)-2-(hydroxyimino)ethyl)sulfanyl)benzoate