High-throughput screening in natural product drug discovery in Australia utilising Australia's biodiversity

Novel Australian biodiversity is being examined as a potential source of ne w therapeutic agents. Drug discovery begins with attempts to find a molecul e that causes a specific biological response, i.e., a "hit." The trend in d rug discovery is clearly towards rapid, high-throughput screening (HTS) of large libraries of compounds. A particularly attractive option for HTS targ ets that has become available with the ability to clone human genes is to u tilise human targets in the screening process. There is increased probabili ty that the compounds discovered would be more effective in their eventual human target than may be the case for compounds discovered using animal mod els or, indeed, animal gene products. HTS strategies involve screening of c ompound libraries, combinatorial libraries, and natural product extracts. T he limiting factor in HTS is the ability to access large numbers of chemica lly diverse substances. Natural products are the greatest source of structu ral diversity HTS of the unparalleled diversity in natural product extracts thereby offers one of the best chances for discovery of novel lead compoun ds and is complementary to the newly emerging source of compounds provided by combinatorial chemistry. However, the complexity of natural product extr acts brings with it the added effort required to obtain a single pure compo und. Drug Dev. Res. 46:250-254, 1999. (C) 1999 Wiley-Liss, Inc.