Sustainable development of natural product research in drug discovery

Natural products have been the successful source of drugs and provided many therapeutic entities to human health problems. During the past few decades, various multidisciplinary approaches have been made to create new opportunities for finding innovative drugs from natural products in the post-genome era. With continuous advancements in molecular biology, cellular biology and genomics, the number of molecular targets has been significantly increased in high throughput screening. Diversity oriented synthesis in chemogenomics and parallel synthesis in combinatorial chemistry are taking the dominant position for „screen friendly“ libraries in drug discovery. Facing increasing competitions, how to enhance the competitiveness of natural products and ensure their sustainable development are the major challenges for their further integration into contemporary drug R&D process. Current approaches are mainly focused on the integration of high throughput technologies into natural product profiling, the integration of the knowledge in traditional medicine into rational drug screening, the integration of unique biodiversity of natural products into random drug screening, the integration of chemical diversity of natural products into combinatorial synthesis, and the integration of cheminformatics and bioinformatics tools into natural product virtual screening and scaffold hopping. Innovative biotechnologies and the latest achievements in metabolic engineering and genetic modification should significantly improve the production sustainability and efficiency of natural product-derived pharmaceuticals.