Bioactives v bioproducts. The road from discovery to market.

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Quinn, Ronald
Camp, David
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2008
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Christchurch, NZ
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Abstract

The wealth of chemical diversity that has evolved with biological diversity has been used as a source of medicines by indigenous peoples for thousands of years.1,2 Research into natural products reached a peak in the period from 1970-80. Of the 877 small molecule New Chemical Entities (NCEs) arising between 1981 and 2007, around 50% were natural products, derived from, or inspired by them.3 However, by the 1990s research on natural products by the pharmaceutical industry was declining. This decline was due to various factors, including the low throughput of screening/isolation of natural product extracts. Drug discovery turned to high throughput screening of large libraries of pure compounds synthesised via combinatorial chemistry. Because the chemical diversity of these libraries was not always relevant to biological function, this approach was not as successful as hoped. The potential rewards from natural product drug discovery are massive despite being regarded by some as a risky, speculative "fishing expedition" with no guarantee of finding compounds of interest. Timelines, governed by the separation of compounds from extracts using bioassay-guided fractionation, are slower than alternative lead generation strategies. This presentation outlines various process improvements implemented at the Eskitis Institute that have streamlined the conventional biodiscovery paradigm. The efficiency gains facilitate delivery of novel chemical leads from NP screening within timelines expected by big pharma and complement HTS as a lead generation strategy. (1) Brohm, D. Angew. Chem. Int. Ed. Engl. 2002, 41, 307-311. (2) Breinbauer, R.; Vetter, I. R.; Waldmann, H. Angew. Chem., Int. Ed. 2002, 41, 2878-2890. (3) Newman, D. J.; Cragg, G. M.; J. Nat. Prod. Rep. 2007, 70, 461-477.

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Bioactives v bioproducts. The road from discovery to market.
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© 2008 Australian Marine Sciences Association. For information about this conference please refer to the publisher's website or contact the authors.
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Natural Products Chemistry
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