Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome.

@article{Desvergne2013DimerizedLM,
  title={Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome.},
  author={Audrey Desvergne and Emilie Genin and Xavier Mar{\'e}chal and Nerea Gallastegui and Laure Dufau and Nicolas Richy and Michael Groll and Jo{\"e}lle Vidal and Mich{\`e}le Reboud-Ravaux},
  journal={Journal of medicinal chemistry},
  year={2013},
  volume={56 8},
  pages={3367-78}
}
Noncovalent proteasome inhibitors introduce an alternative mechanism of inhibition to that of covalent inhibitors used in cancer therapy. Starting from a noncovalent linear mimic of TMC-95A, a series of dimerized inhibitors using polyaminohexanoic acid spacers has been designed and optimized to target simultaneously two of the six active sites of the eukaryotic 20S proteasome. The homodimerized compounds actively inhibited chymotrypsin-like (Ki = 6-11 nM) and trypsin-like activities, whereas… CONTINUE READING
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