Inhibitors of ER Aminopeptidase 1 and 2: From Design to Clinical Application

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Author(s): Dimitris Georgiadis, Anastasia Mpakali, Despoina Koumantou, Efstratios Stratikos*.

Journal Name: Current Medicinal Chemistry

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Endoplasmic Reticulum aminopeptidase 1 and 2 are two homologous enzymes that help generate peptide ligands for presentation by Major Histocompatibility Class I molecules. Their enzymatic activity influences the antigenic peptide repertoire and indirectly controls adaptive immune responses. Accumulating evidence suggests that these two enzymes are tractable targets for the regulation of immune responses with possible applications ranging from cancer immunotherapy to treating inflammatory autoimmune disease. Here, we review the state-of-the-art in the development of inhibitors of ERAP1 and ERAP2 as well as their potential and limitations for clinical applications.

Keywords: aminopeptidase, antigen processing and presentation, peptide, inhibitor, cancer, autoimmunity, infection, MHC, antigen.

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(E-pub Ahead of Print)
DOI: 10.2174/0929867325666180214111849
Price: $95

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