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

doi:10.1002/anie.200454065

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

The University of Tokyo

Research output: Contribution to journal › Article › peer-review

46 Scopus citations

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 language	English
Pages (from-to)	2834-2837
Number of pages	4
Journal	Angewandte Chemie - International Edition
Volume	43
Issue number	21
DOIs	https://doi.org/10.1002/anie.200454065
State	Published - 17 May 2004
Externally published	Yes

Keywords

Agonists
Biological activity
Carbohydrates
Conformation analysis
Receptors

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10.1002/anie.200454065

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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.",

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

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AU - Tamaruya, Yoko

AU - Suzuki, Masato

AU - Kamura, Goshu

AU - Kanai, Motomu

AU - Hama, Kotaro

AU - Shimizu, Kumiko

AU - Aoki, Junken

AU - Arai, Hiroyuki

AU - Shibasaki, Masakatsu

PY - 2004/5/17

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AB - 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.

KW - Agonists

KW - Biological activity

KW - Carbohydrates

KW - Conformation analysis

KW - Receptors

UR - https://www.scopus.com/pages/publications/3242712299

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DO - 10.1002/anie.200454065

M3 - 記事

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JO - Angewandte Chemie - International Edition

JF - Angewandte Chemie - International Edition

IS - 21

ER -

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

Abstract

Keywords

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