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- Title
Screening for content-the evolution of high throughput.
- Authors
Dove, Alan
- Abstract
In principle, high-throughput screening sounds very straightforward. Combinatorial chemists arrange a set of chemical building blocks into all possible combinations, generating a library of millions of compounds. These are then fed into an automated screening system, often patterned onto silicon chips, to determine which compounds bind to a particular target protein or inhibit a particular enzymatic reaction. The successful compounds, now called 'hits', then enter secondary screens to check a number of parameters, including toxicity to cells, solubility and reactivity with nontarget cellular proteins. The chemicals that pass the secondary screens, dubbed 'leads', are then tested in progressively more complex systems, from cells to whole animals, before Although screening technologies have evolved in recent years, as of August 2003 some observers are starting to wonder whether this strategy will pay off. Indeed, high-throughput screening has done little to remedy the current dearth of drugs, as the numbers of new drugs and targets shrink. The guiding philosophy of high-throughput screening is to fail early, eliminating unpromising compounds before they reach the expensive end of the drug development pipeline.
- Subjects
HIGH throughput screening (Drug development); DRUG development; CHEMICAL terrorism; THERAPEUTIC use of enzymes
- Publication
Nature Biotechnology, 2003, Vol 21, Issue 8, p859
- ISSN
1087-0156
- Publication type
Article
- DOI
10.1038/nbt0803-859