Aminopyrimidine-galactose hybrids are highly selective galectin-3 inhibitors.

ABSTRACT: Galectins are a family of carbohydrate recognition proteins involved in, among other things, modulating cell signalling and cell-environment interactions, giving them roles in several pathologies like cancer and idiopathic lung fibrosis. Hence, developing new galectin inhibitors with high affinity and high selectivity is important to be able to target such diseases. Most existing galectin inhibitors have a disaccharide scaffold, but there has been success as of late in developing monogalactoside inhibitors such as α-arylthioglycosides. Here, we report aminopyrimidine-derivatised galactosides as good galectin-3 inhibitors with affinities down to 1.7 μM and a more than 300-fold selectivity over galectin-1. Mutant studies replacing Arg144 in galectin-3 with lysine and serine support the hypot

SUBMITTER: Dahlqvist A 

PROVIDER: S-EPMC6596385 | biostudies-literature | 2019 Jun

REPOSITORIES: biostudies-literature