Optimising in situ click chemistry: the screening and identification of biotin protein ligase inhibitors

William Tieu, Tatiana P Soares da Costa, Min Yin Yap, Kelly L Keeling, Matthew Charles James Wilce, John Campbell Wallace, Grant William Booker, Steven W Polyak, A D Abell

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A `leaky mutant? (SaBPL-R122G) of Staphylococcus aureus biotin protein ligase (SaBPL) is used to enhance the turnover rate for the reaction of biotin alkyne with an azide to give a triazole. This allows the enzyme to select the optimum triazole-based inhibitor using a library of such azides in a single experiment with greatly improved efficiency and sensitivity of detection, difficulties that can restrict the general utility of a multi-component in situ click approach to ligand optimisation.
Original languageEnglish
Pages (from-to)3533 - 3537
Number of pages5
JournalChemical Science
Issue number9
Publication statusPublished - 2013

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