Abstract
Introduction
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 diversityoriented synthesis
- Chemical genetics strategies and tools: simultaneous target and
lead discovery, diversityoriented 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
Mentioned in This Spectrum Report
Companies
- Abbott Laboratories
- Affymetrix
- Ambit Biosciences
- Amgen
- AstraZeneca
- Avalon Pharmaceuticals
- Biogen Idec
- Bristol-Myers Squibb
- Broad Institute
- Cellzome
- CGI Pharmaceuticals
- CombinatoRx
- Exelixis
- GlaxoSmithKline
- Infi nity Pharmaceuticals
- Johnson & Johnson
- Kosan Biosciences
- Novartis
- Pfi zer
- Sanofi -Aventis
- Schering-Plough
- Serenex
- Synta Pharmaceuticals
- Vertex Pharmaceuticals
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