ERAP Inhibitors in Autoimmunity and Immuno-Oncology: Medicinal Chemistry Insights.

ABSTRACT: Endoplasmic reticulum aminopeptidases ERAP1 and 2 are intracellular aminopeptidases that trim antigenic precursors and generate antigens presented by major histocompatibility complex class I (MHC-I) molecules. They thus modulate the antigenic repertoire and drive the adaptive immune response. ERAPs are considered as emerging targets for precision immuno-oncology or for the treatment of autoimmune diseases, in particular MHC-I-opathies. This perspective covers the structural and biological characterization of ERAP, their relevance to these diseases and the ongoing research on small-molecule inhibitors. We describe the chemical and pharmacological space explored by medicinal chemists to exploit the potential of these targets given their localization, biological functions, and family depth. S

SUBMITTER: Fougiaxis V 

PROVIDER: S-EPMC11284793 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature