Glycinamide ribonucleotide transformylase (GAR TFase) as a target for cancer therapy

Cancer of all types is the second leading cause of death in the United States. While there are many different treatment options, antimetabolites inhibit aberrant cell growth by interfering with the formation or utilization of a normal cellular metabolite. Most antimetabolites interfere with the enzymes responsible for DNA synthesis or are incorporated into newly formed DNA, or both. Some antimetabolites are analogues of important cofactors, including the folates. Antifolates have been discovered, synthesized and evaluated that are capable of inhibiting glycinamide ribonucleotide transformylase (GAR TFase), an enzyme within the de novo purine biosynthetic pathway, The establishment and further characterization of GAR TFase as a target for cancer therapy will be reviewed herein.