Acute leukemia is the most aggressive hematological disorder that can be further divided into acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). Current treatment protocols for acute leukemia 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 treatments. 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.