title: Native MS: an 'ESI' way to support structure- and fragment-based drug discovery.
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.
authors.affiliation: NovAliX Structural Biology, Bioparc, Boulevard Sebastien Brant, Illkirch 67400, France. vv@novalix-pharma.com
authors.forename: Valerie
authors.initials: V
authors.lastname: Vivat Hannah
authors.forename: C
authors.initials: C
authors.lastname: Atmanene
authors.forename: D
authors.initials: D
authors.lastname: Zeyer
authors.forename: A
authors.initials: A
authors.lastname: Van Dorsselaer
authors.forename: Sarah
authors.initials: S
authors.lastname: Sanglier-Cianférani
mesh_terms: D055808:Drug Discovery / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D008024:Ligands; D046911:Macromolecular Substances / Q000737:chemistry; D013058:Mass Spectrometry / Q000379:methods*; D008958:Models, Molecular; D015394:Molecular Structure; D011487:Protein Conformation; D011506:Proteins / Q000737:chemistry / Q000378:metabolism; D054852:Small Molecule Libraries; D021241:Spectrometry, Mass, Electrospray Ionization / Q000379:methods*; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D046911:Macromolecular Substances; D011506:Proteins; D054852:Small Molecule Libraries