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Barry R. O'Keefe, Ph.D.
Acting Chief, Molecular Targets Program, Center for Cancer Research
Chief, Natural Products Branch, Developmental Therapeutics Program. Division of Cancer Treatment and Diagnosis
National Cancer Institute
Natural Product-based Drug Discovery: Why, How and Is Now the Time?
The US National Cancer Institute’s Natural Product Extract Repository
Natural products have a proven track record in use as anti-cancer and anti-infective agents. As of 2014 natural products (NP), NP pharmacophores, and NP mimics represented more than 50 percent of small molecule-based anti-cancer and anti-microbial drugs. However, accessing the potential of NPs in high-throughput screening (HTS) campaigns has been challenging due to the complexity of the crude NP extracts, the time necessary for follow-up isolation efforts, and indefinite capabilities for large-scale resupply. This has resulted in NP-based libraries being significantly underrepresented in most recent large-scale HTS programs.
The US National Cancer Institute’s Natural Product Extract Repository is one of the world’s largest, most diverse collections of natural products containing over 230,000 unique extracts derived from plant, marine and microbial organisms. To address the challenges in screening NPs and encourage increased assay of NP chemical diversity, we have initiated the NCI Program for Natural Product Discovery (NPNPD) which has developed an automated, high-throughput robotics platform capable of generating a library of >1,000,000 partially purified extracts for screening. In addition, automated secondary purification and structure elucidation platforms have been created that significantly decrease costs and timelines. This presentation will discuss the reasons for, challenges to, and mechanisms by which to increase the pace and efficiency of NP-based drug discovery.
Fireside Chats with Academic Spin-Outs
Kayothera and Manzara
Scientific Case Studies
Business Panel Discussion
Featuring Daiichi Sankyo, Celgene, MPM Capital and BridgeBio