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 journalArticlepeer-review

15 Citations (Scopus)

Abstract

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

Original languageEnglish
Pages (from-to)242-244
Number of pages3
JournalChemical Communications
Volume47
Issue number1
DOIs
Publication statusPublished - 2011

Keywords

  • 2-AMINOETHOXYDIPHENYL BORATE 2-APB
  • CALCIUM-RELEASE
  • MYOINOSITOL 1,4,5-TRISPHOSPHATE
  • 5-PHOSPHONATE ANALOGS
  • PARTIAL AGONISTS
  • CA2+ RELEASE
  • DERIVATIVES
  • PATHWAY
  • BINDING
  • NAADP

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