Natural Products: Are we close to the end?
The motivation – Natural products are broadly defined as small molecules derived from natural sources. For decades, natural products have played a central role in the discovery and development of modern medicines. This study aimed to explore the structural diversity of compounds isolated from the natural world, and to ask a number of key questions about the state of natural products research, including:
- How has the rate of discovery of new natural products progressed over the past 70 years?
- Has natural product structural novelty changed as a function of time?
- Has the rate of novel natural product discovery declined in recent years?
- Does examining different types of organisms afford an advantage in terms of novel compound discovery?
- Is it possible to estimate how close we are to having described all of the chemical space covered by natural products?
- And finally, is there still value in exploring natural products as a source of novel biologically active natural products?
The discovery – A consortium of researchers from Simon Fraser University, the University of California San Diego and the University of California Santa Cruz used chemoinformatics approaches to explore trends in compound discovery as a function of year of investigation and type of organism. The results demonstrated that, although many novel and interesting compounds continue to be isolated from the environment, this is accompanied by an increasing percentage of 'me too' compounds that are related to previous discoveries. The conclusions from this work suggest that innovative approaches are required if natural products are to contribute to the discovery of the next generation of therapeutic leads.
Its significance – This work provides a clear view of the current situation with regard to novel compound discovery rates from Nature, and provides a perspective on the likely continued success of this discovery model. In addition, it provides insight into the value of various discovery approaches, and offers the science community some perspective on future avenues of investigation. The work has the potential to impact academic and industrial groups interested in natural products research, in both basic science and biotechnology.
Read the paper – “Retrospective analysis of natural products provides insights for future discovery trends” by Cameron R. Pye, Matthew J. Bertin, R. Scott Lokey, William H. Gerwick, Roger G. Linington. Proc. Natl. Acad. Sci. U.S.A Published online 1 May 2017. doi:10.1073/pnas.1614680114.
Website article compiled by Jacqueline Watson with Theresa Kitos