The most significant advantage of proteomic technology is its ability to profile a whole proteome or subproteome in a single experiment, so that the protein alterations corresponding to a pathological or biochemical condition at a given time can be annotated in an integrated way. In oncology and pharmacology these technologies led to the identification of biological markers, which may provide the starting point for the identification of diagnostic markers and therapeutic targets; thus greatly broadening our knowledge and accelerating our path in medical research. In combination with other new technologies in immunology and chemistry, proteomics shows significant potential to make considerable contribution to the drug development process. This article provides a brief overview of the integrative oncoproteomics strategies for anticancer drug discovery, including comparative proteomics, signaling proteomics, membrane proteomics, immunoproteomics and chemistry-based functional proteomics.