6-Mercaptopurine: An Inhibitor of Purine Ribonucleotides and DNA/RNA Synthesis
6-Mercaptopurine (6-MP) is the first effective agent for leukemia, developed by Elion and Hitchings in 1950s. They shared the Nobel Prize in 1988. In cell, 6-MP is converted to 6-thioinosine monophosphate (TIMP), catalyzed by hypoxanthine guanine phosphoribosyltransferase (HPRT). TIMP inhibits conversion of inosinic acid to adenylosuccinic acid and xanthylic acid, subsequently leading to inhibition of purine ribonucleotides and DNA/RNA synthesis. Azathioprine [
A2069] is a prodrug of 6-MP, and both are commonly used as an immunosuppressant for treatment of Crohn’s and inflammatory bowel disease. (The product is for research purpose only.)