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A common single nucleotide polymorphism in endoplasmic reticulum aminopeptidase 2 induces a specificity switch that leads to altered antigen processing.
Evnouchidou I, Birtley J, Seregin S, Papakyriakou A, Zervoudi E, Samiotaki M, Panayotou G, Giastas P, Petrakis O, Georgiadis D, Amalfitano A, Saridakis E, Mavridis IM, Stratikos E. Evnouchidou I, et al. Among authors: giastas p. J Immunol. 2012 Sep 1;189(5):2383-92. doi: 10.4049/jimmunol.1200918. Epub 2012 Jul 25. J Immunol. 2012. PMID: 22837489 Free PMC article.
Crystal Structures of ERAP2 Complexed with Inhibitors Reveal Pharmacophore Requirements for Optimizing Inhibitor Potency.
Mpakali A, Giastas P, Deprez-Poulain R, Papakyriakou A, Koumantou D, Gealageas R, Tsoukalidou S, Vourloumis D, Mavridis IM, Stratikos E, Saridakis E. Mpakali A, et al. Among authors: giastas p. ACS Med Chem Lett. 2017 Feb 21;8(3):333-337. doi: 10.1021/acsmedchemlett.6b00505. eCollection 2017 Mar 9. ACS Med Chem Lett. 2017. PMID: 28337326 Free PMC article.
Mechanism for antigenic peptide selection by endoplasmic reticulum aminopeptidase 1.
Giastas P, Mpakali A, Papakyriakou A, Lelis A, Kokkala P, Neu M, Rowland P, Liddle J, Georgiadis D, Stratikos E. Giastas P, et al. Proc Natl Acad Sci U S A. 2019 Dec 26;116(52):26709-26716. doi: 10.1073/pnas.1912070116. Epub 2019 Dec 16. Proc Natl Acad Sci U S A. 2019. PMID: 31843903 Free PMC article.
Discovery of Selective Nanomolar Inhibitors for Insulin-Regulated Aminopeptidase Based on α-Hydroxy-β-amino Acid Derivatives of Bestatin.
Vourloumis D, Mavridis I, Athanasoulis A, Temponeras I, Koumantou D, Giastas P, Mpakali A, Magrioti V, Leib J, van Endert P, Stratikos E, Papakyriakou A. Vourloumis D, et al. Among authors: giastas p. J Med Chem. 2022 Jul 28;65(14):10098-10117. doi: 10.1021/acs.jmedchem.2c00904. Epub 2022 Jul 14. J Med Chem. 2022. PMID: 35833347
Discovery of the First Selective Nanomolar Inhibitors of ERAP2 by Kinetic Target-Guided Synthesis.
Camberlein V, Fléau C, Sierocki P, Li L, Gealageas R, Bosc D, Guillaume V, Warenghem S, Leroux F, Rosell M, Cheng K, Medve L, Prigent M, Decanter M, Piveteau C, Biela A, Eveque M, Dumont J, Mpakali A, Giastas P, Herledan A, Couturier C, Haupenthal J, Lesire L, Hirsch AKH, Deprez B, Stratikos E, Bouvier M, Deprez-Poulain R. Camberlein V, et al. Among authors: giastas p. Angew Chem Int Ed Engl. 2022 Sep 26;61(39):e202203560. doi: 10.1002/anie.202203560. Epub 2022 Aug 19. Angew Chem Int Ed Engl. 2022. PMID: 35904863 Free PMC article.
35 results