ArticleChemistry & biology2011
Titration-based screening for evaluation of natural product extracts: identification of an aspulvinone family of luciferase inhibitors.
Article in Chemistry & biology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
19 citing papers in PubMed.
- Mapping the structural dynamics of red- and blue-emitting beetle luciferases revealed by HDX-MS.Life science alliance · 2026Article
- Structural and functional insights into δ-poly-L-ornithine polymer biosynthesis from Acinetobacter baumannii.Communications biology · 2023Article
- Quantitative Bioactivity Signatures of Dietary Supplements and Natural Products.ACS pharmacology & translational science · 2023Article
- Molecular Networking and Cultivation Profiling Reveals Diverse Natural Product Classes from an Australian Soil-Derived FungusMolecules (Basel, Switzerland) · 2022Article
- Identification of 2-Benzylidene-tetralone Derivatives as Highly Potent and Reversible Firefly Luciferase Inhibitors.ACS medicinal chemistry letters · 2022Article
- Discovery of GOT1 Inhibitors from a Marine-DerivedMarine drugs · 2021Article
- Evaluation of Firefly andInternational journal of molecular sciences · 2021Article
- The elusive relationship between structure and colour emission in beetle luciferases.Nature reviews. Chemistry · 2021Review
- Aspulvinones Suppress Postprandial Hyperglycemia as Potent α-Glucosidase Inhibitors FromFrontiers in chemistry · 2021Article
- Beetle luciferases with naturally red- and blue-shifted emission.Life science alliance · 2018Article
- The 9Frontiers in cellular and infection microbiology · 2018Article
- Development and Implementation of an HTS-Compatible Assay for the Discovery of Selective Small-Molecule Ligands for Pre-microRNAs.SLAS discovery : advancing life sciences R & D · 2018Article
- Actinoramide A Identified as a Potent Antimalarial from Titration-Based Screening of Marine Natural Product Extracts.Journal of natural products · 2015Article
- Spatial regulation of a common precursor from two distinct genes generates metabolite diversity.Chemical science · 2015Article
- Bioconversion of 6-Tetrahedron letters · 2015Article
- UPLC-MS-ELSD-PDA as a powerful dereplication tool to facilitate compound identification from small-molecule natural product libraries.Journal of natural products · 2014Article
- High-throughput screen of natural product extracts in a yeast model of polyglutamine proteotoxicity.Chemical biology & drug design · 2014Article
- Matching the power of high throughput screening to the chemical diversity of natural products.Natural product reports · 2013Review
- Firefly luciferase in chemical biology: a compendium of inhibitors, mechanistic evaluation of chemotypes, and suggested use as a reporter.Chemistry & biology · 2012Article
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
The chemical diversity of nature has tremendous potential for the discovery of molecular probes and medicinal agents. However, sensitivity of HTS assays to interfering components of crude extracts derived from plants, and macro- and microorganisms has curtailed their use in lead discovery. Here, we describe a process for leveraging the concentration-response curves 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 improves the probability that labor-intensive subsequent steps of reculturing, 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.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.