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Identifying Specific Conformations by Using a Carbohydrate Scaffold: Discovery of Subtype‐Selective LPA‐Receptor Agonists and an Antagonist
Author(s) -
Tamaruya Yoko,
Suzuki Masato,
Kamura Goshu,
Kanai Motomu,
Hama Kotaro,
Shimizu Kumiko,
Aoki Junken,
Arai Hiroyuki,
Shibasaki Masakatsu
Publication year - 2004
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200454065
Subject(s) - lysophosphatidic acid , antagonist , chemistry , carbohydrate , acceptor , receptor , hydrogen bond , stereochemistry , small molecule , molecule , biochemistry , organic chemistry , physics , condensed matter physics
Stable and potent subtype‐selective lysophosphatidic acid (LPA) analogues (agonists and an antagonist) were developed by using carbohydrates as a core structure (see scheme). An array of molecules with the recognition motifs of LPA (a phosphate anion, an oleoyl group, and a hydrogen‐bond acceptor) attached to carbohydrate isomers in different three‐dimensional arrangements were tested for LPA‐receptor activation or inhibition. R=alkyl.