Hirayama Aya, Shirota Osamu, Nomura Mitsuru, Nagadoi Aritaka, Nishimura Yoshifumi
Shiseido Material Science Research Center, Tsuzuki-ku, Yokohama, Kanagawa, Japan.
Anal Biochem. 2006 Jun 1;353(1):99-107. doi: 10.1016/j.ab.2006.03.024. Epub 2006 Apr 19.
A sample-treating system for nuclear magnetic resonance (NMR)-based interaction screening between drug candidates (small molecules) and a protein of interest was developed by applying high-performance liquid chromatography (HPLC) technology. The system prepares a test solution by mixing a (15)N-labeled protein solution and a solution of each candidate compound, loads it to a flow cell-type NMR probe, and recycles the protein after the data acquisition. The system was designed to behave differently according to the information obtained in NMR measurements. In a test operation with a 100-compound library, the system could single out known interacting substances properly. Recovery values of the protein and one representative compound were 75 and 71%, respectively, and the recovered protein was found intact as intended.
通过应用高效液相色谱(HPLC)技术,开发了一种基于核磁共振(NMR)的候选药物(小分子)与目标蛋白之间相互作用筛选的样品处理系统。该系统通过混合(15)N标记的蛋白质溶液和每种候选化合物的溶液来制备测试溶液,将其加载到流通池型NMR探针中,并在数据采集后回收蛋白质。该系统设计为根据NMR测量中获得的信息表现出不同的行为。在对100种化合物文库的测试操作中,该系统能够正确筛选出已知的相互作用物质。蛋白质和一种代表性化合物的回收率分别为75%和71%,并且发现回收的蛋白质按预期保持完整。