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Creating and screening natural product libraries
Brice A P Wilson1, Christopher C Thornburg, Curtis J Henrich
1Molecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702-1201, USA. okeefeba@mail.nih.gov.
Abstract:
Covering: up to 2020The National Cancer Institute of the United States (NCI) has initiated a Cancer Moonshot program entitled the NCI Program for Natural Product Discovery. As part of this effort, the NCI is producing a library of 1 000 000 partially purified natural product fractions which are being plated into 384-well plates and provided to the research community free of charge. As the first 326 000 of these fractions have now been made available, this review seeks to describe the general methods used to collect organisms, extract those organisms, and create a prefractionated library. Importantly, this review also details both cell-based and cell-free bioassay methods and the adaptations necessary to those methods to productively screen natural product libraries. Finally, this review briefly describes post-screen dereplication and compound purification and scale up procedures which can efficiently identify active compounds and produce sufficient quantities of natural products for further pre-clinical development.
Insights
The National Cancer Institute (NCI) is creating a large library of natural product fractions for cancer research. This review details methods for library creation, screening, and identifying potential drug compounds.
Area of Science:
- Natural Product Chemistry
- Drug Discovery
- Cancer Research
Background:
- The National Cancer Institute (NCI) initiated the Cancer Moonshot program, including the NCI Program for Natural Product Discovery.
- A library of 1,000,000 partially purified natural product fractions is being generated and distributed to researchers.
- The first 326,000 fractions are now available, supporting cancer drug discovery efforts.
Purpose of the Study:
- To describe the methods for collecting organisms, extraction, and creating a prefractionated natural product library.
- To detail cell-based and cell-free bioassay methods suitable for screening these natural product libraries.
- To outline post-screen dereplication, compound purification, and scale-up procedures for preclinical development.
Main Methods:
- Organism collection and extraction protocols.
- Development of prefractionated natural product libraries in 384-well plates.
- Adaptation of cell-based and cell-free bioassays for high-throughput screening.
- Procedures for dereplication, purification, and scale-up of active natural products.
Main Results:
- A comprehensive review of methodologies for natural product library generation and screening.
- Detailed description of bioassay adaptations for efficient screening of natural product fractions.
- Outline of strategies for identifying and producing potential anti-cancer compounds.
Conclusions:
- The NCI Program for Natural Product Discovery provides a valuable resource for cancer research.
- Standardized methods facilitate the creation and screening of large natural product libraries.
- Efficient workflows enable the identification and development of novel natural product-based therapeutics.
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