A human metabolic map of pharmacological perturbations reveals drug modes of action

ABSTRACT: Understanding a small molecule’s mode of action (MoA) is essential to guide the selection, optimization and clinical development of lead compounds. In this study, we used high-throughput non-targeted metabolomics to profile changes in 2,269 putative metabolites induced by 1,520 drugs in A549 lung cancer cells. Although only 26% of the drugs inhibited cell growth, 86% caused intracellular metabolic changes, which were largely conserved in two additional cancer cell lines. Using more tan 3.4 million drug–metabolite tested dependencies, we generated a lookup table of drug interference with metabolism, enabling high-throughput characterization of compounds across drug therapeutic classes in a single-pass screen. The identified metabolic changes revealed previously unknown effects of drugs, exp

ORGANISM(S): Homo sapiens (human)

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PROVIDER: S-BSST1724 | biostudies-other |

REPOSITORIES: biostudies-other