My research focuses on applying systems biochemical approaches including novel Stable Isotope-Resolved Metabolomic (SIRM), metabolomics-edited transcriptomic (META), and proteomic approaches (METPA) which we have developed 1) to investigate the anticancer mechanism of natural products and novel therapeutic agents; 2) to explore the functional role(s) of tumor microenvironment and extrinsic environmental factors in cancer development, progression, and therapy; 3) to uncover novel therapeutic targets and distinct mechanism-informed biochemical marker patterns for human diseases by interrogating the human metabolome; and 4) to decipher the gene networks that govern cancer metabolism. The central tool that I have used to achieve these goals is the integration of nuclear magnetic resonance (NMR) with mass spectrometry (MS) technologies, which enables a systematic interrogation of human metabolic networks and their perturbations by diseases.