科研之友
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摘要
Synthesis of doubly 3-O-coumarylmethyl-substituted, thiodigalactosides from bis-3-O-propargyl-thiodigalactoside resulted in, highly selective and high affinity galectin-3 inhibitors. Mutant studies structural analysis and molecular modeling revealed that the coumaryl substituents stack onto arginine side chains. One inhibitor displayed:: efficacy in a murine model of bleomycin-induced lung fibrosis similar to that of a known nonselective galectin-1/galectin-3 inhibitor, which Strongly suggests that blocking galectin-3 glycan recognition is an important antifibrotic drug target.
- 出版日期2016-9-8
