Differential gene regulation and targeted therapy are the critical aspects of several cancers. This book covers specific gene regulation and targeted therapies in different malignancies. It offers a comprehensive assessment of the transcriptional dysregulation in cancer, and considers some examples of transcriptional regulators as definitive oncogenic drivers in solid tumors, followed by a brief discussion of transcriptional effectors of the programs they drive, and discusses its specific targets. Most targeted therapeutics developed to date have been directed against a limited set of oncogenic drivers, exemplified by those encoding cell surface or cytoplasmic kinases that function in intracellular signaling cascades.