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Structure-inspired design of a sphingolipid mimic sphingosine-1-phosphate receptor agonist from a naturally occurring sphingomyelin synthase inhibitor
Title: | Structure-inspired design of a sphingolipid mimic sphingosine-1-phosphate receptor agonist from a naturally occurring sphingomyelin synthase inhibitor |
Authors: | Swamy, Mahadeva M. M. Browse this author | Murai, Yuta Browse this author | Ohno, Yusuke Browse this author →KAKEN DB | Jojima, Keisuke Browse this author | Kihara, Akio Browse this author →KAKEN DB | Mitsutake, Susumu Browse this author →KAKEN DB | Igarashi, Yasuyuki Browse this author →KAKEN DB | Yu, Jian Browse this author | Yao, Min Browse this author →KAKEN DB | Suga, Yoshiko Browse this author | Anetai, Masaki Browse this author | Monde, Kenji Browse this author →KAKEN DB |
Issue Date: | 21-Nov-2018 |
Publisher: | Royal Society of Chemistry |
Journal Title: | Chemical communications |
Volume: | 54 |
Issue: | 90 |
Start Page: | 12758 |
End Page: | 12761 |
Publisher DOI: | 10.1039/c8cc05595e |
Abstract: | Ginkgolic acid obtained as a sphingomyelin synthase inhibitor from a plant extract library inspired the concept of sphingolipid mimics. Ginkgolic acid-derived N-acyl anilines and ginkgolic acid 2-phosphate (GA2P) respectively mimic ceramide and sphingosine 1-phosphate (S1P) in structure and function. The GA2P-induced phosphorylation of ERK and internalization of S1P receptor 1 (S1P(1)) indicated potent agonist activity. Docking studies revealed that GA2P adopts a similar binding conformation to the bound ligand ML5, which is a strong antagonist of S1P(1). |
Type: | article (author version) |
URI: | http://hdl.handle.net/2115/76161 |
Appears in Collections: | 生命科学院・先端生命科学研究院 (Graduate School of Life Science / Faculty of Advanced Life Science) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)
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Submitter: 門出 健次
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