Leukemia is a heterogeneous clonal disease of malignant blood cells. The disease is characterized by a block of differentiation and enhanced proliferation and survival due to genetic abnormalities. Depending on the disease progression, leukemia can be broadly classified into two subtypes: acute leukemia and chronic leukemia. Acute leukemia has been further divided into acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). Acute leukemia is the most aggressive hematological disorder accounting for around 140,000 new cases each year around the world. Current treatment protocols for acute leukemia include induction chemotherapy which is capable of inducing remission in around 75% patients followed by a consolidation treatment and bone marrow transplantation. The overall survival in childhood ALL has reached about 80%, but when considering all risk groups, it is still below 50%. In AML, the overall survival rate is still less than 35%. Therefore, we still need to improve our current treatment beyond that of the current chemotherapeutic approaches. Use of targeted therapy through enhanced understanding of the molecular genetics of leukemogenesis will provide better treatment for the high-risk group of patients. The PI3K/mTOR pathway is one of the central pathway deregulated in acute leukemia. We are exploring the mechanism of PI3K/mTOR pathway upregulation in acute leukemia and also of targeting components of this pathway as possible drug targets.