Kleinberg M L, Wanke L A
Professional Services, Immunex, Seattle, WA 98101, USA.
Am J Health Syst Pharm. 1995 Jun 15;52(12):1323-36; 1341-3. doi: 10.1093/ajhp/52.12.1323.
Traditional and novel approaches to drug design and screening techniques and strategies are described, and the potential benefits of new technologies are discussed. Sophisticated new approaches and technologies in the discovery and design of new drugs are replacing the traditional methods. Rational or structure-based methods of drug design and discovery that integrate techniques of x-ray crystallography, computational chemistry, and nuclear magnetic resonance spectroscopy are becoming the predominant methods. New technologies and methods for drug screening may yield significant savings in time and money, as well as increased diversity and specificity of lead compounds. Intense research activity is now being focused on small-molecule structure-based drug design, in which drugs would mimic the complex molecular interactions of natural proteins. The new approaches and technologies hold promise for dramatic therapeutic advances, particularly in the areas of transcriptionally active drugs and gene therapy. Rapid advances in drug design and screening, brought about through new technologies, may yield significant therapeutic advances and cost-effective therapies.
文中描述了药物设计和筛选技术及策略的传统方法与新方法,并讨论了新技术的潜在益处。新药发现与设计中的先进新方法和技术正在取代传统方法。整合了X射线晶体学、计算化学和核磁共振光谱技术的合理或基于结构的药物设计与发现方法正成为主流方法。药物筛选的新技术和方法可能会大幅节省时间和金钱,同时提高先导化合物的多样性和特异性。目前,大量研究活动集中在基于小分子结构的药物设计上,在这种设计中,药物将模拟天然蛋白质的复杂分子相互作用。这些新方法和技术有望带来显著的治疗进展,特别是在转录活性药物和基因治疗领域。通过新技术实现的药物设计和筛选的快速进展可能会带来显著的治疗进展和具有成本效益的疗法。