Lipids from dietary sources or from de novo synthesis are transported while bound to proteins to other tissues where they are used for cell membrane synthesis or stored for energy generation. In cell membranes or in plasma, lipids can undergo several modifications that are important in cell function. Several proteins orchestrate the transport, biosynthesis, and modification of lipids. Thus, the intersection of lipids and proteins is important in human metabolic pathways. Recent advances in mass spectrometry and bioinformatics have made it possible to obtain compositional (structural and functional) data of lipid molecular species and proteins in biological samples. This combination of lipidomics and proteomics is advantageous because it allows us to better define biochemical pathways, discover new drug targets, and better understand the pathophysiology of several diseases.