Natural Products Genomics: A novel approach for the discovery of anti-cancer therapeutics

N. R. Monks, B. Li, S. Gunjan, D. T. Rogers, M. Kulshrestha, D. L. Falcone, J. M. Littleton

Research output: Contribution to journalArticlepeer-review

11 Scopus citations


Plants continue to retain some advantages over combinatorial chemistry as sources of novel compounds, for example, they can generate metabolites with a complexity beyond synthetic chemistry. However, this comes with its own problems in production and synthetic modification of these compounds. Natural Products Genomics (NPG) aims to access the plants own genomic capacity to increase yields, and modify complex bioactive metabolites, to alleviate these limitations. NPG uses a combination of gain of function mutagenesis and selection to a) mimic the evolution of novel compounds in plants, and b) to increase yields of known bioactive metabolites. This process is performed rapidly at the cell culture level in large populations of mutants. Two examples demonstrating proof of concept in Nicotiana tabacum (tobacco) and proof of application in the medicinal plant species Catharanthus roseus, are included to illustrate the feasibility of this approach. This biotechnology platform may alter the way in which plant drug discovery is perceived by the pharmaceutical industry, and provides an alternative to combinatorial chemistry for the discovery, modification and production of highly complex bioactive molecules.

Original languageEnglish
Pages (from-to)217-225
Number of pages9
JournalJournal of Pharmacological and Toxicological Methods
Issue number3
StatePublished - Nov 2011

Bibliographical note

Funding Information:
The authors would like to thank Dr Philippe Gros (Department of Biochemistry, McGill University, Montreal, Canada) for providing the isogenic HeLa cell lines (HeLa-pcDNA6 and HeLa-MRP1) and Patrick Richardson (Van Andel Research Institute) for his assistance with the statistical analysis.


  • Activation Tagging Mutagenesis
  • Directed elicitation
  • Directed evolution
  • High-Throughput Differential Screening
  • Natural Products Genomics
  • Vinca alkaloids

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology


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