Various N-substituted derivatives of glutamine, asparagine, glutaramic, succinamic and maleamic acids have been synthesized and tested in vitro against Plasmodium falciparum. From these compounds, only the glutamine derivatives (1-3) were found to have low activity. Kinetic evaluation of 1-3 revealed that these compounds also act as competitive inhibitors of gamma-glutamyl transpeptidase (EC 2.3.2.2).
INDOLINE SCAFFOLD SHP-2 INHIBITORS AND METHOD OF TREATING CANCER
申请人:Wu Jie
公开号:US20120034186A1
公开(公告)日:2012-02-09
Protein tyrosine phosphatase (PTP) Shp2 is a non-receptor PTP that involved in cell signaling and regulation of cell proliferation, differentiation, and migration. Shp2 mediates activation of kinases that are involved in the pathogenesis of human carcinoma. A high throughput screen identified compounds that inhibit the PTP Shp2. Several compounds were identified that selectively inhibit Shp2 over Shp1 with low to sub-micromolar activity. Also disclosed are methods of inhibiting a protein tyrosine phosphatase in a cell and treating cancer through selective inhibition of Shp2.
US7645771B2
申请人:——
公开号:US7645771B2
公开(公告)日:2010-01-12
US8623906B2
申请人:——
公开号:US8623906B2
公开(公告)日:2014-01-07
[EN] INDOLINE SCAFFOLD SHP-2 INHIBITORS AND METHOD OF TREATING CANCER<br/>[FR] INHIBITEURS D'ÉCHAFAUDAGE D'INDOLINE SHP-2 ET PROCÉDÉ DE TRAITEMENT DU CANCER
申请人:H LEE MOFFIT CANCER CT AND RES
公开号:WO2010121212A2
公开(公告)日:2010-10-21
Protein tyrosine phosphatase (PTP) Shp2 is a non-receptor PTP that involved in cell signaling and regulation of cell proliferation, differentiation, and migration. Shp2 mediates activation of kinases that are involved in the pathogenesis of human carcinoma. A high throughput screen identified compounds that inhibit the PTP Shp2. Several compounds were identified that selectively inhibit Shp2 over Shp1 with low to sub-micromolar activity. Also disclosed are methods of inhibiting a protein tyrosine phosphatase in a cell and treating cancer through selective inhibition of Shp2.