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Abstract | Cited by

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 InsP3receptor (InsP3R) agonist activity; the compounds that possess a methylphosphonate or a carboxymethyl moiety are InsP3R antagonists.

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

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