Publication

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

Bersellini, M. & Roelfes, G. 14-Apr-2017 In : Organic & Biomolecular Chemistry. 15, 14, p. 3069-3073 5 p.

Research output: Scientific - peer-reviewArticle

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  • Multidrug resistance regulators (MDRs) as sca ff olds for the design of arti fi cial metalloenzymes

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DOI

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.

Original languageEnglish
Pages (from-to)3069-3073
Number of pages5
JournalOrganic & Biomolecular Chemistry
Volume15
Issue number14
StatePublished - 14-Apr-2017

    Keywords

  • BIS(OXAZOLINYL)PYRIDINE-SCANDIUM(III) TRIFLATE COMPLEXES, FRIEDEL-CRAFTS ALKYLATIONS, UNNATURAL AMINO-ACIDS, TRANSCRIPTIONAL REPRESSOR, METAL-BINDING, GENETIC INCORPORATION, PROTEIN, LMRR, QACR, RECOGNITION

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