Cvijic Mary Ellen, Chen Jing, Kubala Steve, Nolfo Joseph, Kolodin Garrett, Zhang Litao
Department of Lead Evaluation, Bristol-Myers Squibb Company, Princeton, New Jersey 08543, USA.
J Lab Autom. 2012 Aug;17(4):266-74. doi: 10.1177/2211068212442502. Epub 2012 Apr 13.
The drug discovery process is dependent on the ability of screening efforts to identify and optimize lead compounds with therapeutic potential. Because G-protein-coupled receptors (GPCRs) account for the most "druggable" targets, the development of high-throughput, low-cost, and high-density GPCR assays to accommodate the increasing size of compound collections is significant. In this study, we report the application of an advanced LEADseeker robotic platform equipped with customized IT solutions for rapid data transfer to reduce assay cycles times for support of GPCR panel screening. The advantages of assay throughput, format, automation design, data management flow, and data reproducibility are discussed in terms of gains in productivity for lead optimization. The GPCR robotic platform demonstrates how automation technology can leverage traditional drug discovery processes by providing consistent and reliable data packages to expedite lead optimization efforts.
药物发现过程依赖于筛选工作识别和优化具有治疗潜力的先导化合物的能力。由于G蛋白偶联受体（GPCRs）是最具“可成药”性的靶点，因此开发高通量、低成本和高密度的GPCR检测方法以适应不断增加的化合物库规模具有重要意义。在本研究中，我们报告了一种先进的LEADseeker机器人平台的应用，该平台配备了定制的IT解决方案以实现快速数据传输，从而减少检测周期时间，以支持GPCR面板筛选。从先导优化的生产力提升方面讨论了检测通量、形式、自动化设计、数据管理流程和数据重现性的优势。GPCR机器人平台展示了自动化技术如何通过提供一致且可靠的数据包来加快先导优化工作，从而利用传统的药物发现过程。
