Cancer kinome is now well organized as an important target for a new class of cancer drugs. There are more than 500 members in the kinase family in which some of them are clinically analysed, while the rest are under investigation for potential therapeutic applications. Phosphorylation, major function of kinases is one of the most significant signal transduction mechanism in which intercellular signals regulate intracellular processes like ion transport, hormone responses and cellular proliferation. Any deregulation of kinase function may lead to tumor progression and other disorders such as immunological, neurological , metabolic including also infectious diseases. This led to the necessity in the development of kinase inhibitors as therapeutic agent. Herein we discuss about different types of kinases and their inhibitors in various types of cancers. This review portrays a broad overview of the origin of kinases, discovery, the characterization and mode of action of kinase inhibitors in cancer therapy.