Discovery of an orally available potent ER aminopeptidase 1 (ERAP1) inhibitor that enhances anti-tumor responses and limits inflammatory autoimmunity in vivo.
Christopher P. Tinworth, Justyna Wojno, Michael Adam…·Efstratios Stratikos
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National and Kapodistrian University of AthensORCID 0000-0002-3566-2309Unclaimed ORCID profile · follow to get notified of new preprints
5 papers
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Christopher P. Tinworth, Justyna Wojno, Michael Adam…·Efstratios Stratikos
Martha Nikopaschou, Martina K. Samiotaki, Anna Kannavou…·Efstratios Stratikos
The paper investigates how ERAP1 allotypes 2 and 10 affect the immunopeptidome of melanoma cells, finding quantitative changes in peptide abundance rather than sequence differences.
Martha Nikopaschou, Martina K. Samiotaki, Elli-Anna Stylianaki…·Efstratios Stratikos
This study shows that ERAP1 inhibition alters the immunopeptidome and proteome in cancer cells, affecting metabolism and stress responses, but only a small fraction of proteomic changes impact the immunopeptidome.
Galateia Georgaki, Anastasia Mpakali, Myrto Trakada…·Efstratios Stratikos
This study investigates the enzymatic properties of ERAP1 allotype 10, showing that polymorphisms V349M and Q725R significantly affect its activity, kinetics, and thermodynamics compared to allotype 1.
Anastasia Mpakali, Galateia Georgaki, Alberto Buson…·Efstratios Stratikos
This paper identifies a nanomolar inhibitor of IRAP that stabilizes its open conformation, revealing a conformation-specific mechanism of action and insights into its catalytic cycle.