Journal
DRUG DISCOVERY TODAY
Volume 28, Issue 10, Pages -Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2023.103751
Keywords
lipids; metabolites; lipidomics; metabolomics; biomarkers; drug discovery and development; mass; spectrometry; clinical trials; target engagement; precision medicine
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Metabolomics and lipidomics play a crucial role in drug discovery and development by providing functional insights through monitoring changes in metabolites and lipids, and promising a transformative impact on precision medicine.
Metabolomics and lipidomics have an increasingly pivotal role in drug discovery and development. In the context of drug discovery, monitoring changes in the levels or composition of metabolites and lipids relative to genetic variations yields functional insights, bolstering human genetics and (meta) genomic methodologies. This approach also sheds light on potential novel targets for therapeutic intervention. In the context of drug development, metabolite and lipid biomarkers contribute to enhanced success rates, promising a transformative impact on precision medicine. In this review, we deviate from analytical chemist-focused perspectives, offering an overview tailored to drug discovery. We provide introductory insight into state-of-the-art mass spectrometry (MS)-based metabolomics and lipidomics techniques utilized in drug discovery and development, drawing from the collective expertise of our research teams. We comprehensively outline the application of metabolomics and lipidomics in advancing drug discovery and development, spanning fundamental research, target identification, mechanisms of action, and the exploration of biomarkers.
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