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Full-Text Articles in Physical Sciences and Mathematics
The Discovery And Study Of Fluvirucin B1 Polyketide Synthase, Tsung-Yi Lin
The Discovery And Study Of Fluvirucin B1 Polyketide Synthase, Tsung-Yi Lin
Doctoral Dissertations
Rapidly decreasing numbers of viable therapeutic leads in the pharmaceutical pipeline demand new, sustainable methods for improved drug discovery and development. Despite vast improvements in de novo drug design and target recognition, Nature remains the richest source of small molecule therapeutics. Among many natural products, polyketides are not only the most promising ones for developing new antibiotic leads, but also exhibit unusually high therapeutic value ranging from clinical use as anticancer, antiviral, and immunosuppressant drugs. Modular polyketide synthases (PKSs) are dedicated nano-machinery that can be manipulated to produce a structurally diverse library for drug discovery programs. The ability to manipulate …
Reactive Probes For Manipulating Polyketide Synthases, And Photoreactive Probes For Strained Alkyne Click Chemistry, Jon William Amoroso
Reactive Probes For Manipulating Polyketide Synthases, And Photoreactive Probes For Strained Alkyne Click Chemistry, Jon William Amoroso
Doctoral Dissertations
Polyketides are a broad class of natural products that have received attention from the scientific community because they are a rich mine of bioactive structures. The common thread that binds the class together is the method by which they are synthesized, by large enzymatic complexes called polyketide synthases (PKSs) which display assembly line like organization. A great deal of effort has been put into studying PKSs, but their mechanistic steps are still not perfectly understood. In order to further the study of PKSs and their components, we have developed a series of reactive small molecules that covalently modify specific sites …