Identifying specific conformations by using a carbohydrate scaffold: Discovery of subtype-selective LPA-receptor agonists and an antagonist

Yoko Tamaruya, Masato Suzuki, Goshu Kamura, Motomu Kanai, Kotaro Hama, Kumiko Shimizu, Junken Aoki, Hiroyuki Arai, Masakatsu Shibasaki

Research output: Contribution to journalArticlepeer-review

40 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)2834-2837
Number of pages4
JournalAngewandte Chemie - International Edition
Volume43
Issue number21
DOIs
Publication statusPublished - 2004 May 17
Externally publishedYes

Keywords

  • Agonists
  • Biological activity
  • Carbohydrates
  • Conformation analysis
  • Receptors

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)

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