Author/Authors :
Laszlo Revesz، نويسنده , , Ernst Blum، نويسنده , , Ute Manning، نويسنده , , B. Jachez Demange، نويسنده , , Armin Widmer، نويسنده , , Jean-François Zuber، نويسنده ,
Abstract :
Non-peptide bidentate ITAM mimics as ZAP-70 antagonists have been prepared by accommodating non-hydrolyzable phosphotyrosine analogues at each end of a non-peptide spacer with a maximal P-P distance of 39 Å. The most potent antagonist 5 had an IC50=0.25μM against ZAP-70 with good cellular activity. Monodentates were ca. 10-fold weaker antagonists with improved cell permeability.