Table of Contents
- Executive Summary
- Strategic Considerations
- Stakeholder Implications
- Introduction to Chemical Genetics: The Chemistry-First Strategy
- Basics of Chemical Genetics
- Chemical Genetics Strategies and Tools
- Simultaneous Target and Lead Discovery
- Diversity-Oriented Synthesis Libraries
- Chemoproteomics Strategies
- Agonists and Reversal of Loss-of-Function
- Enabling Technologies for Chemical Genetics
- The NIH Molecular Libraries Roadmap
- Molecular Libraries Screening Center Network
- PubChem
- Technology Development
- Expectations of the MLR Initiative
- Chemical Genetics for Drug Discovery
- Cellular Phenotypic Screens
- CombinatoRx
- CGI Pharmaceuticals
- Synta Pharmaceuticals
- Model Organisms
- Cellular Gene Expression Screens
- Avalon Pharmaceuticals
- GlaxoSmithKline
- The Broad Institute
- Chemoproteomics and Chemogenomics Methods
- Schering-Plough' s Automated Ligand Identification System
- High-Throughput Kinase Screening at Exelixis and Vertex
- Ambit Biosciences' KinomeScan
- Serenex' s Affinity-Based Chemoproteomics Platform
- Cellzome' s Chemical Proteomics Technology
- Outlook for Chemical Genetics
Tables
- 1. Potential Advantages of Chemical Genetics Strategies and Approaches
- 2. Enabling Technologies for Chemical Genetics
- 3. Select Companies Utilizing Cellular or Whole-Organism Phenotypic Screen
Technologies for Chemical Genetics
- 4. Companies Utilizing Chemoproteomics or Chemogenomics Technologies
- 5. Select Small-Molecule Agents Discovered Using Chemical Genetics
Figures
- 1. Chemical Genetic Strategy to Discover Compounds That Reverse PTEN
Loss-of-Function
- 2. CGI Pharmaceuticals' Analogue Sensitive Kinase Alleles (ASKA) Technology
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