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A comparative kinetic characterization of the peptide aldehydes Ac-Leu-Leu-X-H [X = Trp, Tyr and Tyr(tBu)] and Z-Gly-Pro-Gly-Gly-Leu-Leu-Nle-H as inhibitors of the chymotryptic activity of 20S proteasomes from the archaebacterium T. acidophilum and yeast S. cerevisiae revealed significantly differentiated inhibitory potencies that can be rationalized on the basis of X-ray crystallographic data.

biological chemistry

Synthesis, Kinetic Characterization and X-Ray Analysis of Peptide Aldehydes as Inhibitors of the 20S Proteasomes from  Thermoplasma acidophilum  and  Saccharomyces cerevisiae