Development of inositol-based antagonists for the d-myo-inositol 1,4,5-trisphosphate receptor

Neil S. Keddie; Yulin Ye; Tashfeen Aslam; Tomas Luyten; Davide Bello; Clive Garnham; Geert Bultynck; Antony Galione; Stuart J. Conway

doi:10.1039/c0cc03003a

Development of inositol-based antagonists for the d-myo-inositol 1,4,5-trisphosphate receptor

Neil S. Keddie, Yulin Ye, Tashfeen Aslam, Tomas Luyten, Davide Bello, Clive Garnham, Geert Bultynck, Antony Galione, Stuart J. Conway

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

Abstract

The syntheses of four d-myo-inositol 1,4,5-trisphosphate (InsP3) derivatives, incorporating phosphate bioisosteres at the 5-position, are reported. The methyl phosphate ester and sulfate derivatives retain InsP 3 receptor (InsP3R) agonist activity; the compounds that possess a methylphosphonate or a carboxymethyl moiety are InsP3R antagonists. © 2011 The Royal Society of Chemistry.

Original language	English
Pages (from-to)	242-244
Number of pages	2
Journal	Chemical Communications
Volume	47
Issue number	1
DOIs	https://doi.org/10.1039/c0cc03003a
Publication status	Published - 7 Jan 2011

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abstract = "The syntheses of four d-myo-inositol 1,4,5-trisphosphate (InsP3) derivatives, incorporating phosphate bioisosteres at the 5-position, are reported. The methyl phosphate ester and sulfate derivatives retain InsP 3 receptor (InsP3R) agonist activity; the compounds that possess a methylphosphonate or a carboxymethyl moiety are InsP3R antagonists. {\textcopyright} 2011 The Royal Society of Chemistry.",

author = "Keddie, {Neil S.} and Yulin Ye and Tashfeen Aslam and Tomas Luyten and Davide Bello and Clive Garnham and Geert Bultynck and Antony Galione and Conway, {Stuart J.}",

note = ", Biotechnology and Biological Sciences Research Council, United Kingdom",

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T1 - Development of inositol-based antagonists for the d-myo-inositol 1,4,5-trisphosphate receptor

AU - Keddie, Neil S.

AU - Ye, Yulin

AU - Aslam, Tashfeen

AU - Luyten, Tomas

AU - Bello, Davide

AU - Garnham, Clive

AU - Bultynck, Geert

AU - Galione, Antony

AU - Conway, Stuart J.

N1 - , Biotechnology and Biological Sciences Research Council, United Kingdom

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AB - The syntheses of four d-myo-inositol 1,4,5-trisphosphate (InsP3) derivatives, incorporating phosphate bioisosteres at the 5-position, are reported. The methyl phosphate ester and sulfate derivatives retain InsP 3 receptor (InsP3R) agonist activity; the compounds that possess a methylphosphonate or a carboxymethyl moiety are InsP3R antagonists. © 2011 The Royal Society of Chemistry.

U2 - 10.1039/c0cc03003a

DO - 10.1039/c0cc03003a

M3 - Article

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SP - 242

EP - 244

JO - Chemical Communications

JF - Chemical Communications

IS - 1

ER -

Development of inositol-based antagonists for the d-myo-inositol 1,4,5-trisphosphate receptor

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