Abstract: Technology advancements in the past decades have enabled the systemic characterization of lipids using integrative approaches, a discipline which is termed "lipidomics". This review summarizes suitable methodologies to discover, identify and quantitatively monitor lipids in biological systems. The emphasis is put on the understanding of interactions between cellular components, in particular the lipid-protein interrelationships. Various tools and techniques for probing lipid-protein interactions will be discussed. It is expected that by integrating the approaches of lipidomics, transcriptomics and proteomics, a clear understanding of the complex functions of lipids will eventually be translated into human health and diseases.