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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