Diphenylfuropyrimidine (DFP) analogs are broadly active against primary Nef-mediated Hck activation.

Abstract

<p>A) Structures of 4-amino DFP (DFP-4A) and the corresponding 4-aminopropanol (DFP-4AP) and 4-aminobutanol (DFP-4AB) analogs. B) The activity of recombinant downregulated Hck (Hck-YEEI) <a href="http://www.plosone.org/article/info:doi/10.1371/journal.pone.0032561#pone.0032561-Trible1" target="_blank">[44]</a>, <a href="http://www.plosone.org/article/info:doi/10.1371/journal.pone.0032561#pone.0032561-Trible2" target="_blank">[52]</a>, <a href="http://www.plosone.org/article/info:doi/10.1371/journal.pone.0032561#pone.0032561-EmertSedlak1" target="_blank">[53]</a> was determined in the absence or presence of the indicated Nef proteins as described under <a href="http://www.plosone.org/article/info:doi/10.1371/journal.pone.0032561#s3" target="_blank">Materials and Methods</a>. Reactions were run in the presence of 10 µM concentrations of DFP-4A, DFP-4AP, DFP-4AB, or the DMSO carrier solvent as negative control. Results are expressed as the mean percent of maximum substrate phosphorylation ± S.D.; this experiment was repeated twice with comparable results.</p