Activation of IP3 receptors by synthetic bisphosphate ligands

Kana M. Sureshan, Andrew M. Riley, Ana M. Rossi, Stephen C. Tovey, Skarlatos G. Dedos, Colin W. Taylor, Barry V. L. Potter

Research output: Contribution to journalArticlepeer-review

26 Citations (SciVal)


Ca2+ release by D-myo-inositol 1,4,5-trisphosphate receptors (IP(3)Rs) is widely considered to require the vicinal 4,5-bisphosphate motif of IP3, with P-5 and P-4 engaging the alpha and beta domains of the binding site; using synthesis and mutagenesis we show that the adenine of synthetic glyconucleotides, through an interaction with Arg504, can replace the interaction of either P-1 or P-5 with the alpha-domain producing, respectively, the most potent bisphosphate agonist yet synthesised and the first agonist of IP3R without a vicinal bisphosphate motif; this will stimulate new approaches to IP3R ligand design.
Original languageEnglish
Pages (from-to)1204-1206
JournalChemical Communications
Issue number10
Early online date4 Feb 2009
Publication statusPublished - 14 Mar 2009


Dive into the research topics of 'Activation of IP3 receptors by synthetic bisphosphate ligands'. Together they form a unique fingerprint.

Cite this