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市場調查報告書
藥物開發的遺傳生化學
Chemical Genetics in Drug Discovery
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本報告已在2011年12月21日停止出版。
在趨向藥物開發過程合理化之中，生物科技企業及製藥企業已經開始運用遺傳生化學來克服傳統藥物開發的瓶頸。
廣泛調查醫療業界的美國專業市調公司 Decision Resources Inc. （總公司：麻州），調查與分析藥物開發的遺傳生化學，並有系統地出版綜合報告書 "Chemical Genetics in Drug Discovery"。
此報告書使用24頁的篇幅，除了說明遺傳生化學的基本知識與策略及工具、遺傳生化學技術導入至藥物開發的動向，也探討化學性蛋白質體學與化學基因體學手法、及遺傳生化學的未來展望等。此報告書的概略架構如下所示。
摘要
遺傳生化學的說明
遺傳生化學的基礎
遺傳生化學策略與工具
- 目標與線索的同時發現
- 多樣化的合成資料庫
- 化學性蛋白質體學策略
- 作動藥與功能損失的恢復
- 遺傳生化學技術
NIH Molecular Libraries藍圖
- Molecular Libraries Screening Center Network
- PubChem
- 技術開發
- MLR主導權的期待
藥物開發的遺傳生化學
- 細胞表現型篩選
- CombionatoRx
- CGI Phamaceuticals
- Synta Pharmaceuticals
- 樣本生物
- 細胞基因發現篩選
- Avalon Pharmaceuticals
- GlaxoSmithKline
- The Broad Institute
- 化學性蛋白質體學及化學基因體學的手法
- Schering-Plough的自動配體特定系統
- Exelixis、Vertex的高通路Kinase篩選
- Ambit Biosciences的KinomeScan
- Serenex的相似化學性蛋白質體學平台
- Cellzome的化學蛋白質抗體技術
遺傳生化學的未來展望
表
- 遺傳生化學策略與研究的優點
- 遺傳生化學的可能技術
- 使用遺傳生化學的細胞或生物表現型篩選技術的企業
- 使用化學性蛋白質體學或化學基因體學技術的企業
- 利用遺傳生化學發現的小分子劑
圖
- 為發現可以恢復PTEN功能損失的化合物的遺傳生化學策略
- CGI Pharmaceuticals的ASKA技術
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
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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