Non-peptide ITAM mimics as ZAP-70 antagonists

Article abstract of DOI:10.1016/S0960-894X(97)10102-0

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 A. 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.