Activation of IP3 receptors by synthetic bisphosphate ligands

Reference:

Sureshan, K. M., Riley, A. M., Rossi, A. M., Tovey, S. C., Dedos, S. G., Taylor, C. W. and Potter, B. V. L., 2009. Activation of IP3 receptors by synthetic bisphosphate ligands. Chemical Communications

Related documents:

Official URL:

http://dx.doi.org/10.1039/b819328b

Related URLs:

• http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2898634/

Abstract

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.

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