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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

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

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

Volume 26, Issue 15, 2019

Page: [2715 - 2729] Pages: 15

DOI: 10.2174/0929867325666180214111849

Price: $65


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 diseases. 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: Immune system, antigen, peptide, enzyme, inhibitor, cancer, autoimmunity, infection.

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