Cancer is uncontrolled cell growth guided by deregulation of cell growth network. Subsequently, alteration in genes occurs which influences expression (down-regulation of tumor suppressor genes and/or up-regulation of proto-oncogene) of these prominent cell growth proteins. Protein targeting has emerged as a hope against cancer. These therapies work by inhibiting or up regulating the target proteins through agents specific for treatment of deregulated proteins. Targeted cancer therapies are more favorable for cancers like lung, colorectal, breast, lymphoma and leukemia as they focus on particular molecular changes unique to a specific cancer. As researchers scrutinize and comprehend the cell changes that initiate cancer, they are better able to design promising therapies targeting these changes or nullify their effect. In present study we have assessed prospects of significant proteins which are known to be targeted by number of small molecules and related drugs for effective treatment of various forms of cancer. Moreover, we also addressed the efficacies of these drugs toward the cancer treatment and future challenges in their development as this information is lacking in previously published work.