Sureshan, Kana M. ; Riley, Andrew M. ; Rossi, Ana M. ; Tovey, Stephen C. ; Dedos, Skarlatos G. ; Taylor, Colin W. ; Potter, Barry V. L. (2009) Activation of IP3 receptors by synthetic bisphosphate ligands Chemical Communications (10). p. 1204. ISSN 1359-7345
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Official URL: http://doi.org/10.1039/B819328B
Related URL: http://dx.doi.org/10.1039/B819328B
Abstract
Ca2+ release by D-myo-inositol 1,4,5-trisphosphate receptors (IP3Rs) is widely considered to require the vicinal 4,5-bisphosphate motif of IP3, with P-5 and P-4 engaging the α and β 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 α-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.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Royal Society of Chemistry. |
| ID Code: | 119869 |
| Deposited On: | 18 Jun 2021 04:13 |
| Last Modified: | 18 Jun 2021 04:13 |
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