A re-examination of the difluoromethylenesulfonic acid group as a phosphotyrosine mimic for PTP1B inhibition
M Hussain, V Ahmed, B Hill, Z Ahmed…
文献索引：Hussain, Munawar; Ahmed, Vanessa; Hill, Bryan; Ahmed, Zaheer; Taylor, Scott D. Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 14 p. 6764 - 6777
Protein tyrosine phosphatase 1B (PTP1B) is involved in the down-regulation of insulin signaling and is a well-validated therapeutic target for the treatment of diabetes and obesity. Key to the design of potent inhibitors of PTP1B is a moiety that effectively mimics the phosphate group of the natural phosphotyrosine substrate. Difluoromethylsulfonomethylphenylalanine (F2Smp) is one of the best monoanionic pTyr ...
