Activation of IP(3) receptors by synthetic bisphosphate ligands.
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ABSTRACT:
SUBMITTER: Sureshan KM
PROVIDER: S-EPMC2898634 | biostudies-literature | 2009 Mar
REPOSITORIES: biostudies-literature
Publications
Activation of IP(3) receptors by synthetic bisphosphate ligands.
Sureshan Kana M KM Riley Andrew M AM Rossi Ana M AM Tovey Stephen C SC Dedos Skarlatos G SG Taylor Colin W CW Potter Barry V L BV
Chemical communications (Cambridge, England) 20090204 10
Ca(2+) 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 IP(3), 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 ...[more]
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