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ID: ALA1136136
Journal: Bioorg Med Chem Lett
Title: Formylchromone derivatives as a novel class of protein tyrosine phosphatase 1B inhibitors.
Authors: Shim YS, Kim KC, Chi DY, Lee KH, Cho H.
Abstract: Formylchromone inhibits a human protein tyrosine phosphatase PTP1B with a IC(50) value of 73 microM. The chemical reactivity of formylchromone was adjusted by substitution at various positions of the formylchromone skeleton. In an initial assessment of the structure-activity relationship, the most potent inhibitor showed an IC(50) of 4.3 microM against PTP1B and strong or medium selectivity against other human PTPases, LAR and TC-PTP. This compound, however, was not selective against microbial PTPases, YPTP1 and YOP. The potency and selectivity of the formylchromone derivatives expecting further improvements provides a novel pharmacophore for the design of drugs for the treatment of type 2 diabetes and obesity.
CiteXplore: 12852966