Inhibitors of the advanced glycosylation of proteins and methods of use therefor.

摘要

The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with a carbonyl moiety of an early glycosylation product of such target proteins resulting from their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. The agents comprise compounds having the following structural formula: R1-CH2-R2 (I) wherein R1 is -CN, or <CHEM> R2 is the same as R1, or additionally can be -SO2R, <CHEM> R is a lower alkyl group; R3 is R, -OH, -OR, -NH2, -NHNH2, -NHR; with the proviso that when R1 and R2 are independently selected from <CHEM> wherein R3 is R, -OR or -NHR, then the lower alkyl portion may be an alkanediyl bridge of 1-5 carbon atoms joining the molecule into a cyclic structure; their pharmaceutically acceptable acid addition salts; and a carrier therefor. . T