NovAliX Structural Biology, Bioparc, Boulevard Sebastien Brant, Illkirch 67400, France.
Future Med Chem. 2010 Jan;2(1):35-50. doi: 10.4155/fmc.09.141.
The success of early drug-discovery programs depends on the adequate combination of complementary and orthogonal technologies allowing hit/lead compounds to be optimized and improve therapeutic activity. Among the available biophysical methods, native MS recently emerged as an efficient method for compound-binding screening. Native MS is a highly sensitive and accurate screening technique. This review provides a description of the general approach and an overview of the possible characterization of ligand-binding properties. How native MS supports structure- and fragment-based drug research will also be discussed, with examples from the literature and internal developments. Native MS shows strong potential for in-depth characterization of ligand-binding properties. It is also a reliable screening technique in drug-discovery processes.
早期药物发现计划的成功取决于互补和正交技术的充分结合，这些技术可使命中/先导化合物得到优化并提高治疗活性。在现有的生物物理方法中，天然 MS 最近成为一种用于化合物结合筛选的有效方法。天然 MS 是一种高度灵敏和准确的筛选技术。本文综述了一般方法，并概述了配体结合特性的可能表征。还将讨论天然 MS 如何支持基于结构和基于片段的药物研究，以及文献和内部开发的实例。天然 MS 具有深入表征配体结合特性的强大潜力。它也是药物发现过程中的可靠筛选技术。
