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Publication - Professor Jonathan Clayden

    End-to-end conformational communication through a synthetic purinergic receptor by ligand-induced helicity switching

    Citation

    Brown, RA, Diemer, V, Webb, SJ & Clayden, J, 2013, ‘End-to-end conformational communication through a synthetic purinergic receptor by ligand-induced helicity switching’. Nature Chemistry, vol 5., pp. 853-860

    Abstract

    The long-range communication of information, exemplified by signal transduction through membrane-bound receptors, is a central biochemical function. Reversible binding of a messenger ligand induces a local conformational change that is relayed through the receptor, inducing a chemical effect typically several nanometres from the binding site. We report a synthetic receptor mimic that transmits structural information from a boron-based ligand binding site to a spectroscopic reporter located more than 2 nm away. Reversible binding of a diol ligand to the N-terminal binding site induces a screw-sense preference in a helical oligo(aminoisobutyric acid) foldamer, which is relayed to a reporter group at the remote C-terminus, communicating information about the structure and stereochemistry of the ligand. The reversible nature of boronate esterification was exploited to switch the receptor sequentially between left- and right-handed helices, while the exquisite conformational sensitivity of the helical relay allowed the reporter to differentiate even between purine and pyrimidine nucleosides as ligands.

    Full details in the University publications repository