Research from Q. Dang and colleagues provide new insights into life sciences
2009 JUL 13 - (NewsRx.com) -- "Inhibition of FBPase is. considered a promising way to reduce hepatic gluconeogenesis and therefore could be a potential approach to treat type 2 diabetes. Herein we report the discovery of a series of purine phosphonic acids as AMP mimics targeting the AMP site of FBPase, which was achieved using a structure-guided drug design approach," scientists in the United States report. "These non-nucleotide purine analogues inhibit FBPase in a similar manner and with similar potency as AMP. More importantly, several purine analogues exhibited potent cellular and in vivo glucose-lowering activities, thus achieving proof-of-concept for inhibiting FBPase as a drug discovery target. For example, compounds 4.11 and 4.13 are as equipotent as AMP with regard to FBPase inhibition," wrote Q. Dang and colleagues. The researchers concluded: "Furthermore, compound 4.11 inhibited glucose production in primary rat hepatocytes and significantly lowered blood glucose levels in fasted rats.." Dang and colleagues published their study in the Journal of Medicinal Chemistry (Fructose-1,6-bisphosphatase Inhibitors. 1. Purine Phosphonic Acids as Novel AMP Mimics. Journal of Medicinal Chemistry, 2009;52(9):2880-2898). For more information, contact Q. Dang, Metabasis Therapeutic Inc., Dept. of Med Chemical, 11119 N Torrey Pines Rd., La Jolla, CA 92037, USA. Publisher contact information for the Journal of Medicinal Chemistry is: American Chemical Society, 1155 16th St., NW, Washington, DC 20036, USA. Keywords: United States, La Jolla, Life Sciences, Type 2 Diabetes Mellitus, Non-insulin Dependent Diabetes Mellitus, Enzyme Research, Bisphosphatase, Pharmaceuticals, Drug Development, Therapy, Treatment, Medicinal Chemistry. This article was prepared by Diabetes Week editors from staff and other reports. Copyright 2009, Diabetes Week via NewsRx.com.
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