Crystal Structures of ERAP2 Complexed with Inhibitors Reveal Pharmacophore Requirements for Optimizing Inhibitor Potency

Mpakali, Anastasia; Giastas, Petros; Deprez‐Poulain, Rebecca; Papakyriakou, Athanasios; Koumantou, Despoina; Gealageas, Ronan; Tsoukalidou, Sofia; Vourloumis, Dionisios; M. Mavridis, Irene; Stratikos, Efstratios; Saridakis, Emmanuel

doi:10.1021/acsmedchemlett.6b00505

Public

Crystal Structures of ERAP2 Complexed with Inhibitors Reveal Pharmacophore Requirements for Optimizing Inhibitor Potency

Published in ACS Medicinal Chemistry Letters • Feb 21, 2017

Authors:

Anastasia Mpakali

Petros Giastas

Rebecca Deprez‐Poulain

Abstract

Endoplasmic reticulum aminopeptidase 2 assists with the generation of antigenic peptides for presentation onto Major Histocompatibility Class I molecules in humans. Recent evidence has suggested that the activity of ERAP2 may contribute to the generation of autoimmunity, thus making ERAP2 a possible...

Subject

Pharmacophore

Hydroxamic acid

Binding site

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