An approach to diketone-galectin-3 inhibitor

Abstract: In many biological mechanisms galectins play important roles. The galectins are important in inflammation, immunologic response and cancer. A key function of galectins is cross-linking of their glycoprotein ligands which are connected with the biological activities. Carbohydrate recognition domains (CRD) are responsible for the cross-linking. The galectin CRDs are divided into subsites A-E and it has been discovered that there is a binding affinity for Arg144 in subsite A-B of galectin-3. In a recent study they discovered that diacetyl is binding covalently to N-α-acetylarginine. It is interesting to synthesize a galectin inhibitor with diketone functionality and test if it binds to Arg144.