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ID: ALA1147821

Journal: Bioorg Med Chem Lett

Title: P3 and P4 position analysis of vinyl ester pseudopeptide proteasome inhibitors.

Authors: Marastoni M, Baldisserotto A, Trapella C, Gavioli R, Tomatis R.

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 (beta2) subunit. In both positions, aromatic and hydrophobic residues were preferred.

CiteXplore: 16603348

DOI: 10.1016/j.bmcl.2006.03.070