Marastoni Mauro, Baldisserotto Anna, Cellini Silvia, Gavioli Riccardo, Tomatis Roberto
Department of Pharmaceutical Sciences and Biotechnology Centre, University of Ferrara, I-44100 Ferrara, Italy.
J Med Chem. 2005 Jul 28;48(15):5038-42. doi: 10.1021/jm040905d.
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.
蛋白酶体是一种多催化蛋白酶复合物，在细胞内蛋白质降解中起核心作用。我们在此报告一类对胰蛋白酶样活性具有选择性的新型特异性蛋白酶体抑制剂的合成及其生物学活性。这些带有C端乙烯基酯的基于三肽的化合物无毒，不影响细胞增殖，但能够调节由MHC I类分子呈递的免疫原性肽的产生和呈递。
