87006-36-8Relevant academic research and scientific papers
Selective protein tyrosine phosphatase 1B inhibitors: Targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands
Liu, Gang,Xin, Zhili,Liang, Heng,Abad-Zapatero, Cele,Hajduk, Philip J.,Janowick, David A.,Szczepankiewicz, Bruce G.,Pei, Zhonghua,Hutchins, Charles W.,Ballaron, Stephen J.,Stashko, Michael A.,Lubben, Thomas H.,Berg, Cathy E.,Rondinone, Cristina M.,Trevillyan, James M.,Jirousek, Michael R.
, p. 3437 - 3440 (2007/10/03)
Protein tyrosine phosphatase (PTPase) 1B (PTP1B) has been implicated as a key negative regulator of both insulin and leptin signaling cascades. We identified several salicylic acid-based ligands for the second phosphotyrosine binding site of PTP1B using a NMR-based screening. Structure-based linking with a catalytic site-directed oxalylarylaminobenzoic acid-based pharmacophore led to the identification of a novel series of potent PTP1B inhibitors exhibiting 6-fold selectivity over the highly homologous T-cell PTPase (TCPTP) and high selectivity over other phosphatases.
