Azaserine

Azaserine is a tumor-inhibiting antibiotic isolated from a species of Streptomyces that functions as a glutamine analog.^1,2 At 25 μM, it inhibits the glutamine-dependent amidotransferases involved in nucleotide biosynthesis, phosphoribosylformylglycinamidine synthetase and glucosamine-6-phosphate isomerase.^2,3 Azaserine also inhibits the hexosamine biosynthetic pathway, which shunts excessive intracellular glucose into the biosynthesis of UDP-N-acetylglucosamine and the formation of O-linked glycoproteins.⁴ Azaserine has been shown to protect against hyperglycemic endothelial damage through its antioxidant effects.⁴

WARNING This product is not for human or veterinary use.

1. Wise, D.R., and Thompson, C.B. Glutamine addiction: A new therapeutic target in cancer. Trends Biochem. Sci. 35(8), 427-433 (2010).

2. Lyons, S.D., Sant, M.E., and Christopherson, R.I. Cytotoxic mechanisms of glutamine antagonists in mouse L1210 leukemia. The Journal of Biological Chemisty 265(19), 11377-11381 (1990).

3. King, J.B., West, M.B., Cook, P.F., et al. A novel, species-specific class of uncompetitive inhibitors of γ-glutamyl transpeptidase. The Journal of Biological Chemisty 284(14), 9059-9065 (2009).

4. Rajapakse, A.G., Ming, X.F., Carvas, J.M., et al. The hexosamine biosynthesis inhibitor azaserine prevents endothelial inflammation and dysfunction under hyperglycemic condition through antioxidant effects. Am. J. Physiol. Heart Circ. Physiol. 296(3), H815-H822 (2009).