Two small libraries of tripeptidic-based vinyl ester derivative proteasome inhibitors were synthesized and tested, starting with the Hmb-Val-Gln-Leu-VE prototype. The P3 and P4 positions were investigated with a complete set of amino acid residues, some of which showed remarkable selective inhibition of the trypsin-like (b2) subunit. In both positions, aromatic and hydrophobic residues were preferred.
P3 and P4 position analysis of vinyl ester pseudopeptide proteasome inhibitors
MARASTONI, Mauro;BALDISSEROTTO, Anna;TRAPELLA, Claudio;GAVIOLI, Riccardo;TOMATIS, Roberto
2006
Abstract
Two small libraries of tripeptidic-based vinyl ester derivative proteasome inhibitors were synthesized and tested, starting with the Hmb-Val-Gln-Leu-VE prototype. The P3 and P4 positions were investigated with a complete set of amino acid residues, some of which showed remarkable selective inhibition of the trypsin-like (b2) subunit. In both positions, aromatic and hydrophobic residues were preferred.File in questo prodotto:
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