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Chemical Genetics in Drug Discovery
Decision Resources, Inc., Nov 2006, Pages: 24


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In the drive to streamline the drug discovery process, biotechnology and pharmaceutical companies are harnessing chemical genetics as a tool to overcome the limitations of traditional target-based drug discovery. Although chemical genetics approaches show great potential, their ultimate success can be measured only when drug candidates discovered using these technologies reach the marketplace.

Questions Answered in This Spectrum Report
Although chemical genetics was originally developed for basic biological research, industry has enlisted this approach to improve the effectiveness of small-molecule drug discovery and development. What are the potential advantages of chemical genetics for drug discovery, and how will chemical genetics change the current drug discovery model? What technologies enable its use?
Several drug candidates derived from chemical genetics programs are now in the early stages of development, some of which are first-in-class agents that may have been difficult to discover by other means. Which companies are utilizing chemical genetics strategies, and what promising agents are in their pipelines?
The NIH has launched an initiative to create a comprehensive set of small-molecule compounds that can modulate human genes and their functions, proving that the scientific community believes that chemical genetics has great potential both in biological research and in drug development.
What are the primary aims of the NIH program? How does the program promise to drive innovation in chemical genetics, and what resources will it offer to commercial and academic researchers?

Scope:
- Basics of chemical genetics: development, key aspects, and the central role of diversity oriented synthesis.
- Chemical genetics strategies and tools: simultaneous target and lead discovery, diversity oriented synthesis libraries, chemoproteomics strategies, agonists and reversal of loss-offunction, and enabling technologies for chemical genetics.
- The NIH Molecular Libraries Roadmap: Molecular Libraries Screening Center Network, PubChem, technology development, and expectations of the MLR initiative.
- Chemical genetics for drug discovery: cellular phenotypic screens, model organisms, and cellular gene expression screens.
- Chemoproteomics and chemogenomics methods: approaches involving in vitro affi nity screening of small-molecule compounds against purified proteins.
- Outlook for chemical genetics: the impact of chemical genetics on the drug-discovery programs of pharmaceutical and biotechnology companies.


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