Huber Walter, Mueller Francis
F. Hoffmann-La Roche AG, Department of Pharma Research, CH-4070 Basel, Switzerland.
Curr Pharm Des. 2006;12(31):3999-4021. doi: 10.2174/138161206778743600.
The review gives first an introduction into the basics of surface plasmon resonance technology. The physical principle is shortly discussed followed by a discussion of the experimental details to be considered when using this technology for biomolecular interaction analysis. Based on recent publications it is demonstrated that the technology has widespread applications in many fields of the drug discovery process. Protein/protein interactions can be monitored in real time when working with biopharmaceuticals as well as protein/small analyte interactions during hit finding, secondary screening, lead optimization and lead selection. Equilibrium binding constants, kinetic rate constants and thermodynamic parameters are obtained from such study that helps to understand the mechanism of the binding reactions. This information can be directly used to improve binding properties of a drug candidate.
该综述首先介绍了表面等离子体共振技术的基础知识。简要讨论了其物理原理，随后探讨了将该技术用于生物分子相互作用分析时需考虑的实验细节。基于近期的出版物表明，该技术在药物发现过程的许多领域都有广泛应用。在处理生物制药时可实时监测蛋白质/蛋白质相互作用，以及在先导化合物发现、二次筛选、先导化合物优化和先导化合物选择过程中监测蛋白质/小分子分析物相互作用。通过此类研究可获得平衡结合常数、动力学速率常数和热力学参数，这有助于理解结合反应的机制。这些信息可直接用于改善候选药物的结合特性。
