Non-Thiol farnesyltransferase inhibitors: utilization of an aryl binding site by 5-arylacryloylaminobenzophenones

…, M Böhm, P Wißner, I Sattler, M Schlitzer

Index: Mitsch, Andreas; Boehm, Markus; Wissner, Pia; Sattler, Isabel; Schlitzer, Martin Bioorganic and medicinal chemistry, 2002 , vol. 10, # 8 p. 2657 - 2662

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Citation Number: 17

Abstract

We recently described a novel aryl binding site of farnesyltransferase. The 2- naphthylacryloyl residue was developed as an appropriate substituent for our benzophenone-based AAX-peptidomimetic capable of occupying this binding site, resulting in a non-thiol farnesyltransferase inhibitor with nanomolar activity. The activity of this inhibitor is readily explained on the basis of docking studies which show the 2-naphthyl ...