At present, available therapies are only partially effective in patients with leukemia and the vast majority of patients cannot be cured with current treatment strategies. Hence, there is an obvious need to develop more specific and effective drugs for the treatment of these diseases. In the last twenty years, significant progress in molecular and cellular biology has resulted in a better chara...

•Development of MAT2A inhibitors (MAT2Ai) AGI-24512 and AG-270 with improved potency•AGI-24152 reduce proliferation cancer cells tumors that lack MTAP•MAT2Ai PRMT5 activity affecting mRNA splicing inducing DNA damage•Antiproliferative effects are synergistic taxanes in vitro vivo The methylthioadenosine phosphorylase (MTAP) gene is located adjacent to the cyclin-dependent kinase inhibitor 2A (C...