Titration-based screening for evaluation of natural product extracts: identification of an aspulvinone family of luciferase inhibitors.

@article{Cruz2011TitrationbasedSF,
  title={Titration-based screening for evaluation of natural product extracts: identification of an aspulvinone family of luciferase inhibitors.},
  author={Patricia G Cruz and Douglas S Auld and Pamela J. Schultz and S. Daniel Lovell and Kevin P. Battaile and Ryan Macarthur and Min Shen and Giselle Tamayo-Castillo and James Inglese and David H. Sherman},
  journal={Chemistry & biology},
  year={2011},
  volume={18 11},
  pages={
          1442-52
        }
}
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… CONTINUE READING
Related Discussions
This paper has been referenced on Twitter 1 time. VIEW TWEETS

Citations

Publications citing this paper.
Showing 1-7 of 7 extracted citations

References

Publications referenced by this paper.
Showing 1-10 of 47 references

Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124.

Proceedings of the National Academy of Sciences of the United States of America • 2010
View 4 Excerpts
Highly Influenced

Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries.

Proceedings of the National Academy of Sciences of the United States of America • 2006
View 9 Excerpts
Highly Influenced

Mechanism of PTC124 activity in cell-based luciferase assays of nonsense codon suppression.

Proceedings of the National Academy of Sciences of the United States of America • 2009
View 6 Excerpts
Highly Influenced

A short history of SHELX.

Acta crystallographica. Section A, Foundations of crystallography • 2008
View 2 Excerpts
Highly Influenced

PHENIX: a comprehensive Python-based system for macromolecular structure solution

Acta crystallographica. Section D, Biological crystallography • 2010
View 1 Excerpt