Non-thiol farnesyltransferase inhibitors: utilization of an aryl binding site by 5-arylacryloylaminobenzophenones |
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Authors: | Mitsch Andreas Böhm Markus Wissner Pia Sattler Isabel Schlitzer Martin |
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Institution: | Institut für Pharmazeutische Chemie, Philipps-Universit?t Marburg, Marbacher Weg 6, D-35032 Marburg, Germany. |
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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 residue fitting into the aryl binding site. |
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