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dc.contributor.authorCruz, Patricia G.
dc.contributor.authorAuld, Douglas S.
dc.contributor.authorSchultz, Pamela
dc.contributor.authorLovell, Scott
dc.contributor.authorBattaile, Kevin P.
dc.contributor.authorMacArthur, Ryan
dc.contributor.authorShen, Min
dc.contributor.authorTamayo-Castillo, Giselle
dc.contributor.authorInglese, James
dc.contributor.authorSherman, David H.
dc.identifier.citationCruz, Patricia G., Douglas S. Auld, Pamela J. Schultz, Scott Lovell, Kevin P. Battaile, Ryan Macarthur, Min Shen, Giselle Tamayo-Castillo, James Inglese, and David H. Sherman. "Titration-Based Screening for Evaluation of Natural Product Extracts: Identification of an Aspulvinone Family of Luciferase Inhibitors." Chemistry & Biology 18.11 (2011): 1442-452.en_US
dc.description.abstractThe chemical diversity of nature has tremendous potential for discovery of new molecular probes and medicinal agents. However, sensitivity of HTS assays to interfering components of crude extracts derived from plants, macro- and microorganisms has curtailed their use in lead discovery efforts. Here we describe a process for leveraging the concentration-response curves (CRCs) obtained from quantitative HTS to improve the initial selection of “actives” from a library of partially fractionated natural product extracts derived from marine actinomycetes and fungi. By using pharmacological activity, the first-pass CRC paradigm aims to improve the probability that labor-intensive subsequent steps of re-culturing, extraction and bioassay-guided isolation of active component(s) target the most promising strains and growth conditions. We illustrate how this process identified a family of fungal metabolites as potent inhibitors of firefly luciferase, subsequently resolved in molecular detail by x-ray crystallography.en_US
dc.titleTitration-based screening for evaluation of natural product extracts: identification of an aspulvinone family of luciferase inhibitorsen_US
kusw.kuauthorLovell, Scott
kusw.kudepartmentHiguchi Biosciences Centeren_US
kusw.oaversionScholarly/refereed, author accepted manuscripten_US
kusw.oapolicyThis item meets KU Open Access policy criteria.en_US

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