The proteasome is a multicatalytic proteinase complex which plays a central role in intracellular protein degradation. We report here the synthesis and biological activities of a new class of specific proteasome inhibitors selective for trypsin-like activity. These tripeptide-based compounds bearing a C-terminal vinyl ester are nontoxic, and do not affect cell proliferation, but are able to modulate the generation and presentation of immunogenic peptides presented by MHC class I molecules.
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Univ E Anglia, Norwich Med Sch, Biomed Res Ctr, Norwich NR4 7TJ, Norfolk, EnglandUniv E Anglia, Norwich Med Sch, Biomed Res Ctr, Norwich NR4 7TJ, Norfolk, England
Steverding, Dietmar
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Baldisserotto, Anna
Wang, Xia
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Univ E Anglia, Norwich Med Sch, Biomed Res Ctr, Norwich NR4 7TJ, Norfolk, EnglandUniv E Anglia, Norwich Med Sch, Biomed Res Ctr, Norwich NR4 7TJ, Norfolk, England
Wang, Xia
Marastoni, Mauro
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Univ Ferrara, Dept Pharmaceut Sci, I-44100 Ferrara, Italy
Univ Ferrara, Ctr Biotechnol, I-44100 Ferrara, ItalyUniv E Anglia, Norwich Med Sch, Biomed Res Ctr, Norwich NR4 7TJ, Norfolk, England
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Leiden Univ, Leiden Inst Chem, NL-2333 CC Leiden, NetherlandsUniv East Anglia, Norwich Med Sch, Bob Champion Res & Educ Bldg, Norwich NR4 7UQ, Norfolk, England
Florea, Bogdan I.
Overkleeft, Herman S.
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Leiden Univ, Leiden Inst Chem, NL-2333 CC Leiden, NetherlandsUniv East Anglia, Norwich Med Sch, Bob Champion Res & Educ Bldg, Norwich NR4 7UQ, Norfolk, England