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  • Title: Structure-based design of human immuno- and constitutive proteasomes inhibitors.
    Author: Richy N, Sarraf D, Maréchal X, Janmamode N, Le Guével R, Genin E, Reboud-Ravaux M, Vidal J.
    Journal: Eur J Med Chem; 2018 Feb 10; 145():570-587. PubMed ID: 29339252.
    Abstract:
    Starting from the X-ray structure of our previous tripeptidic linear mimics of TMC-95A in complex with yeast 20S proteasome, we introduced new structural features to induce a differential inhibition between human constitutive and immunoproteasome 20S particles. Libraries of 24 tripeptidic and 6 dipeptidic derivatives were synthesized. The optimized preparation of 3-hydroxyoxindolyl alanine residues from tryptophan and their incorporation in peptides were described. Several potent inhibitors of human constitutive proteasome and immunoproteasome acting at the nanomolar level (IC50 = 7.1 nM against the chymotrypsin-like activity for the best inhibitor) were obtained. A cytotoxic effect at the submicromolar level was observed against 6 human cancer cell lines.
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