蛋白质-配体亲和质谱的最新进展。
Recent developments in protein-ligand affinity mass spectrometry.
机构信息
BioMolecular Analysis, Department of Chemistry and Pharmaceutical Sciences, Faculty of Sciences, VU University Amsterdam, The Netherlands.
出版信息
Anal Bioanal Chem. 2011 Mar;399(8):2669-81. doi: 10.1007/s00216-010-4350-z. Epub 2010 Nov 8.
Abstract
This review provides an overview of direct and indirect technologies to screen protein-ligand interactions with mass spectrometry. These technologies have as a key feature the selection or affinity purification of ligands in mixtures prior to detection. Specific fields of interest for these technologies are metabolic profiling of bioactive metabolites, natural extract screening, and the screening of libraries for bioactives, such as parallel synthesis libraries and small combichem libraries. The review addresses the principles of each of the methods discussed, with a focus on developments in recent years, and the applicability of the methods to lead generation and development in drug discovery.
摘要
本文综述了利用质谱筛选蛋白-配体相互作用的直接和间接技术。这些技术的一个关键特征是在检测之前对混合物中的配体进行选择或亲和纯化。这些技术的特定应用领域包括生物活性代谢物的代谢组学、天然提取物筛选以及用于生物活性物质的文库筛选，如平行合成文库和小分子组合文库。本文讨论了每种方法的原理，并重点介绍了近年来的发展，以及这些方法在药物发现中的先导化合物生成和开发中的适用性。
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