Advances in polyketide synthase structure and function

Research output: Contribution to journalReview articlepeer-review

38 Scopus citations

Abstract

Recent progress in the understanding of polyketide synthase (PKS) continues to fuel the growth of combinatorial biosynthesis for natural product structural diversity. The structural analysis of many components of PKS, in particular for the modular type I 6-deoxyerythronilide B synthase (DEBS) involved in erythromycin biosynthesis, has provided structural imperatives for the observed biochemistry of DEBS and has enabled the generation of a working structural model of the entire DEBS system. New functions for PKS domains continue to be defined, such as the general control nonderepressible 5 (GCN5) N-acyltransferase strategy for polyketide chain initiation and the true identity of the elusive precursor for the methoxymalonylate extender unit. Novel molecular architectures have been continuously uncovered, including the 'AT-less' PKS and enediyne PKS, thereby expanding the known bacterial PKS paradigms beyond the prototypical type I, II and III PKSs. Finally, the genetic characterization of PKS in vivo and biochemical studies of PKS in vitro have also been greatly facilitated by the application of emerging technologies, such as RNA-mediated gene silencing, reconstitution of an entire polyketide biosynthetic pathway in a model heterologous host and Fourier-transform mass spectroscopy. The application of these technologies is discussed.

Original languageEnglish
Pages (from-to)186-195
Number of pages10
JournalCurrent Opinion in Drug Discovery and Development
Volume11
Issue number2
StatePublished - Mar 2008

Funding

FundersFunder number
National Childhood Cancer Registry – National Cancer InstituteR01CA106150

    Keywords

    • 6-Deoxyerythronolide B synthase
    • DEBS
    • Enediynes
    • Fatty acid synthase
    • Natural product biosynthesis
    • Polyketide synthase

    ASJC Scopus subject areas

    • Pharmacology
    • Drug Discovery

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