Title:Inhibitors of ER Aminopeptidase 1 and 2: From Design to Clinical Application
Volume: 26
Issue: 15
Author(s): Dimitris Georgiadis, Anastasia Mpakali, Despoina Koumantou and Efstratios Stratikos*
Affiliation:
- National Center for Scientific Research Demokritos, Agia Paraskevi, 15341,Greece
Keywords:
Immune system, antigen, peptide, enzyme, inhibitor, cancer, autoimmunity, infection.
Abstract: 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.