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Specifically, taking advantage of our understanding of the active epitope of the regulatory NOX1 subunit NOXA1 as a potent inhibitor of NOX1\u2010derived O<jats:sub>2<\/jats:sub>\u22c5<jats:sup>\u2212<\/jats:sup> formation, a panel of peptidomimetic derivatives of this peptide were designed and synthesized with the aim of improving their activity and increasing their stability in plasma. The results highlighted that improved efficacy and potency was found for both the peptide\u2010peptoid hybrid <jats:bold>GS2<\/jats:bold>, whereas stapled peptide <jats:bold>AC5<\/jats:bold> and its precursor showed higher stability despite lower biological potency. 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