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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, 2009 (10), pp. 1204-1206.

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Official URL:

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

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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.

Details

Item Type Articles
CreatorsSureshan, K. M., Riley, A. M., Rossi, A. M., Tovey, S. C., Dedos, S. G., Taylor, C. W. and Potter, B. V. L.
DOI10.1039/b819328b
Related URLs
URLURL Type
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2898634/Free Full-text
DepartmentsFaculty of Science > Pharmacy & Pharmacology
RefereedYes
StatusPublished
ID Code13442

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