Abstract
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.
Acknowledgements
The authors are very thankful to Fabrice Ciesielski, Pascal Muller, Dominique Roecklin and Anne Briot-Dietsch for there contributions to this review. The authors would like to thank the CNRS, the University of Strasbourg UDS, the region Alsace and the French Fondation pour la Recherche Médicale for financial support.
Financial & competing interests disclosure
V Vivat Hannah and D Zeyer are employees of NovAliX. CA was supported by a studentship from the French Ministère de la Recherche. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.
No writing assistance was utilized in the production of this manuscript.