Non-peptide itam mimics as ZAP-70 antagonists

…, U Manning, BJ Demange, A Widmer, JF Zuber

Index: Revesz, Laszlo; Blum, Ernst; Manning, Ute; Demange, B. Jachez; Widmer, Armin; Zuber, Jean-Francois Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 22 p. 2875 - 2878

Full Text: HTML

Citation Number: 8

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 PP distance of 39 Å. The most potent antagonist 5 had an IC50= 0.25 μM against ZAP-70 with good cellular activity. Monodentates were ca. 10-fold weaker antagonists with improved cell permeability.