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  • Title: Immunoproteasome β5i-Selective Dipeptidomimetic Inhibitors.
    Author: Singh PK, Fan H, Jiang X, Shi L, Nathan CF, Lin G.
    Journal: ChemMedChem; 2016 Oct 06; 11(19):2127-2131. PubMed ID: 27561172.
    Abstract:
    N,C-capped dipeptides belong to a class of noncovalent proteasome inhibitors. Herein we report that the insertion of a β-amino acid into N,C-capped dipeptides markedly decreases their inhibitory potency against human constitutive proteasome β5c, while maintaining potent inhibitory activity against human immunoproteasome β5i, thereby achieving thousands-fold selectivity for β5i over β5c. Structure-activity relationship studies revealed that β5c does not tolerate the β-amino acid based dipeptidomimetics as does β5i. In vitro, one such compound was found to inhibit human T cell proliferation. Compounds of this class may have potential as therapeutics for autoimmune and inflammatory diseases with less mechanism-based cytotoxicity than agents that also inhibit the constitutive proteasome.
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