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Issue 14, 2017
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Multidrug resistance regulators (MDRs) as scaffolds for the design of artificial metalloenzymes

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Abstract

The choice of protein scaffolds is an important element in the design of artificial metalloenzymes. Herein, we introduce Multidrug Resistance Regulators (MDRs) from the TetR family as a viable class of protein scaffolds for artificial metalloenzyme design. In vivo incorporation of the metal binding amino acid (2,2-bipyridin-5yl)alanine (BpyA) by stop codon suppression methods was used to create artificial metalloenzymes from three members of the TetR family of MDRs: QacR, CgmR and RamR. Excellent results were achieved with QacR Y123BpyA in the Cu2+ catalyzed enantioselective vinylogous Friedel–Crafts alkylation reaction with ee's up to 94% of the opposite enantiomer that was achieved with other mutants and the previously reported LmrR-based artificial metalloenzymes.

Graphical abstract: Multidrug resistance regulators (MDRs) as scaffolds for the design of artificial metalloenzymes

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Publication details

The article was received on 16 Feb 2017, accepted on 14 Mar 2017 and first published on 14 Mar 2017


Article type: Paper
DOI: 10.1039/C7OB00390K
Citation: Org. Biomol. Chem., 2017,15, 3069-3073
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    Multidrug resistance regulators (MDRs) as scaffolds for the design of artificial metalloenzymes

    M. Bersellini and G. Roelfes, Org. Biomol. Chem., 2017, 15, 3069
    DOI: 10.1039/C7OB00390K

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