AFFINITY IMAGE-INSTRUMENTATION FOR DRUG DISCOVERY

通过筛选组合文库来发现先导药物已经成为许多制药公司的重要任务，由于生产的化合物数量巨大，因此有必要采用池中而不是单独测试文库的方法。智能光学系统，提出了一种快速，廉价的小型化，自动化。高灵敏度、无标记的光学成像仪器（“Affinity Image”），用于在高通量（HTS）和超高通量（UHTS）筛选测定中快速筛选和表征组合文库。拟议的仪器将是非常灵活的，并将有可能进行动态和平衡测定超过4000个不同的目标，同时。由于不需要标记，并且可以同时进行多个测定，因此该仪器代表了该行业在材料和劳动力成本方面的大量节省。亲和图像作为HTS应用程序的工具的可行性将通过模型系统来证明。在该项目的I期期间，将测试两个模型系统：（1）抗-b-内啡肽抗体的表位作图和（2）探测与链霉亲和素的生物素结合位点结合的肽和非肽配体。拟议的商业应用：Affinity Image将是参与药物发现的制药和生物技术行业的主要兴趣。Affinity Image将出售给全球超过275家拥有多个研究地点的制药公司，以及几乎所有其他私人，学术和医学支持的生物分析实验室。

The discovery of drug leads by screening combinatorial libraries has become an important mandate of many pharmaceutical companies.Because of the vast number of compounds produced it is necessary to employ methods for testing the libraries in pools rather than individually. Intelligent Optical Systems, proposes a fast, inexpensive miniaturized, automated. highly sensitive, labelless, optical imaging instrument ("Affinity Image") for rapid screening and characterization of combinatorial libraries in high-throughput (HTS) and ultra high- throughput (UHTS) screening assays. The proposed instrument will be extremely flexible and will have the potential to perform dynamic and equilibrium assays for more than 4000 different targets simultaneously. Since no labels are needed and multiple assays can be performed simultaneously this instrument represents substantial savings in the material and labor costs for the industry. The feasibility of Affinity Image as a tool for HTS applications will be demonstrated with model systems. During Phase I of this project two model systems will be tested: (l) epitope mapping of anti-b-endorphin antibody and (2) probing peptide and nonpeptide ligands that bind to the biotin binding site of streptavidin. PROPOSED COMMERCIAL APPLICATIONS: Affinity Image will be of primary interest to pharmaceutical and biotechnology industries involved in drug discovery. Affinity Image would be sold to more than 275 pharmaceutical companies worldwide with multiple research locations and to virtually all other private, academic, and publically supported bioanalytical laboratories.