Natural Product-Based Drug Discovery
Authors: Rongshi Li
Journal: Medicinal Research Reviews (2015)

It is my great pleasure to introduce the special issue "Natural Product-Based Drug Discovery". When planning this special issue for Medicinal Research Reviews two years ago, our intention was to review natural product-based drug discoveries, advocate and promote collaborative efforts between drug developers, biologists, and organic, medicinal, and natural product chemists to elevate natural product-based drug discovery to new levels. Natural products have provided the most successful supply of new chemical entities (NCEs) for drug discovery in the last 75 years. Natural products, their derivatives, metabolites, and mimics account for about 50% of NCEs developed to treat human diseases. We expect this trend to continue and more success stories to come in the near future. This special issue contains six reviews by leading contributors in the field—primarily from groups in academia, although some authors have had previous experience in the pharmaceutical and biotech industry. The topics in this special issue cover a broad range of research and success stories in natural product-based drug discovery. The issue begins with Cochrane and Vederas who review lipopeptides from Bacillus and Paenibacillus spp. Many of the lipopeptides produced by these bacteria have been known for decades and represent a potential gold mine of antibiotic candidates with a representative structure of tridecaptin A1 shown on the cover. Xiao, Morris-Natschke, and Lee give an overview on strategies for the optimization of natural product leads to anticancer drugs or drug candidates. Khandelwal, Crowley, and Blagg highlight the development of Hsp90 inhibitors as a therapeutic opportunity for the treatment of cancer, as well as the development of clinically important inhibitors from natural products. This is one of the great examples of how organic/medicinal chemists use natural product inhibitors of Hsp90 as leads for the development of more efficacious inhibitors and analogs that have entered clinical trials. Jiang et al. cover the therapeutic potential of steroidal alkaloids in cancer and other diseases. Waterman et al. present an overview on miniaturized cultivation of microbiota for antimalarial drug discovery. Finally, Li gives a comprehensive review of marine natural product-based drug discovery, and the total synthesis, biosynthesis, and analog synthesis of marinopyrroles as inhibitors of Mcl-1/Bcl-xL/MRSA/MRSE. Li also points out potential issues arising from the poor physicochemical properties of marinopyrrole derivatives reported to date and future considerations. At the end, I thank all authors for their outstanding contributions. Next, I thank the many reviewers who spent their valuable time, made diligent efforts, and provided insightful suggestions to improve the quality of these review articles. Furthermore, I specially thank the Editor-in-Chief of Medicinal Research Reviews, Professor Binghe Wang, and the Editorial Office staff for their patience and continuous support of this project. Last but not least, I hope that the readers of Medicinal Research Reviews enjoy this special issue on Natural Product-Based Drug Discovery.