title: Mass spectrometry-based proteomics in preclinical drug discovery.
abstract: Preclinical stages in the drug discovery process require a multitude of biochemical and genetic assays in order to characterize the effects of drug candidates on cellular systems and model organisms. Early attempts to apply unbiased proteomic techniques to the identification of protein targets and off-targets as well as to elucidate the mode of action of candidate drug molecules suffered from a striking discrepancy between scientific expectations and what the technology was able to deliver at the time. Dramatic technological improvements in mass spectrometry-based proteomic and chemoproteomic strategies have radically changed this situation. This review, therefore, highlights proteomic approaches suitable for preclinical drug discovery illustrated by recent success stories.
authors.affiliation: Novartis Institutes for BioMedical Research, Inc., Cambridge, MA 02139, USA. markus.schirle@novartis.com
authors.forename: Markus
authors.initials: M
authors.lastname: Schirle
authors.forename: Marcus
authors.initials: M
authors.lastname: Bantscheff
authors.forename: Bernhard
authors.initials: B
authors.lastname: Kuster
mesh_terms: D000818:Animals; D015415:Biomarkers / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D064420:Drug-Related Side Effects and Adverse Reactions; D013058:Mass Spectrometry; D004364:Pharmaceutical Preparations / Q000378:metabolism; D011485:Protein Binding; D025941:Protein Interaction Mapping; D011506:Proteins / Q000378:metabolism; D040901:Proteomics
chemical_list: D015415:Biomarkers; D004364:Pharmaceutical Preparations; D011506:Proteins