Structure-based Engineering of Enzymes Involved in the Biosynthesis of Secondary Metabolites

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Type III polyketide synthases catalyze the biosynthesis of structurally diverse, biologically active plant polyophenols. On the basis of the X-ray crystal structures of the enzymes, we rationally designed and generated a set of site-directed mutant enzymes with novel and expanded catalytic functions. Further, by exploiting the promiscuous substrate specificities of the enzymes, we succeeded in production of an array of chemically and structurally divergent unnatural novel compounds.