Chemotherapy has been used for treatment of human cancer since early 1900 with purified natural products or synthetic compounds to kill rapidly growing tumor cells or to reduce their growth. However, chemotherapy is also toxic to some rapidly proliferating normal cells such as bone marrow, therefore causing undesirable side effects. With recent advances in molecular biology, genetics, and signaling transduction, many types of cancer can be traced back to mutation(s), abnormal pathway activations, or altered expressions of a molecule, a pathway, and/or a group of proteins, which can be targeted to specifically inhibit cancer cells, but not normal tissues. In 2002, Dr. Charles Sawyers used "Targeted cancer therapy" to review the development in this field for the first time1. In the last decade, cancer drug targets have been extended to signaling pathways, protein–protein complexes, and signaling networks in tumor cells, tumor stromal tissues, and immune systems.