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Article

Discovery of Selective Inhibitors of Endoplasmic Reticulum Aminopeptidase 1.

Journal of medicinal chemistry - 9 Jan 2020

Maben Zachary, Arya Richa, Rane Digamber, An W Frank, Metkar Shailesh, Hickey Marc, Bender Samantha, Ali Akbar, Nguyen Tina T, Evnouchidou Irini, Schilling Roger, Stratikos Efstratios, Golden Jennifer, Stern Lawrence J

Abstract excerpt

ERAP1 is an endoplasmic reticulum-resident zinc aminopeptidase that plays an important role in the immune system by trimming peptides for loading onto major histocompatibility complex proteins. Here, we report discovery of the first inhibitors selective for ERAP1 over its paralogues ERAP2 and IRAP. Compound 1 (N-(N-(2-(1H-indol-3-yl)ethyl)carbamimidoyl)-2,5-difluorobenzenesulfonamide) and compound 2...

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Identifiers

PMID: 31841350
DOI: 10.1021/acs.jmedchem.9b00293
PMCID: PMC8218592

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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