Novel, potent, selective and cellular active ABC type PTP1B inhibitors containing (methanesulfonyl-phenyl-amino)-acetic acid methyl ester phosphotyrosine mimetic

Add time:07/14/2019    Source:sciencedirect.com

Protein tyrosine phosphatase 1B (PTP1B) which plays an important role in the negative regulation of insulin and leptin pathway has emerged as a novel promising therapeutic target for the treatment of type 2 diabetes mellitus and obesity. Upon careful study, a series of novel scaffold and simple synthesis method inhibitors were discovered based on the analysis of X-ray crystal structures of PTP1B/inhibitor complexes and docking simulations. Among them, compound P7 exhibited high inhibitory activity (IC50 = 222 nM) with moderate selectivity (8-fold) over T-cell PTPase (TCPTP) through interacting with the A, B and C binding sites of PTP1B enzyme. Further studies on cellular activities revealed that compound P7 could enhance insulin-mediated IRβ phosphorylation and insulin-stimulated glucose uptake.

We also recommend Trading Suppliers and Manufacturers of 3-(4-METHOXY-BENZENESULFONYLAMINO)-PROPIONIC ACID (cas 59724-72-0). Pls Click Website Link as below: cas 59724-72-0 suppliers

Prev:Design, synthesis, and evaluation of a novel series of α-substituted phenylpropanoic acid derivatives as human peroxisome proliferator-activated receptor (PPAR) α/δ dual agonists for the treatment of metabolic syndrome
Next:Crystal structure of tris(4,4′-dimethoxy-2,2′-bipyridine)iron (II) bis (hexafluorophosphate) , solvate with N-methyl-2-pyrrolidone)