Seeking for non-zinc-binding MMP-2 inhibitors: Synthesis, biological evaluation and molecular modelling studies

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Abstract

Matrix metalloproteinases (MMPs) are an important family of zinc-containing enzymes with a central role in many physiological and pathological processes. Although several MMP inhibitors have been synthesized over the years, none reached the market because of off-target effects, due to the presence of a zinc binding group in the inhibitor structure. To overcome this problem non-zinc-binding inhibitors (NZIs) have been recently designed. In a previous article, a virtual screening campaign identified some hydroxynaphtyridine and hydroxyquinoline as MMP-2 non-zinc-binding inhibitors. In the present work, simplified analogues of previously-identified hits have been synthesized and tested in enzyme inhibition assays. Docking and molecular dynamics studies were carried out to rationalize the activity data.

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Ammazzalorso, A., De Filippis, B., Campestre, C., Laghezza, A., Marrone, A., Amoroso, R., … Agamennone, M. (2016). Seeking for non-zinc-binding MMP-2 inhibitors: Synthesis, biological evaluation and molecular modelling studies. International Journal of Molecular Sciences, 17(10). https://doi.org/10.3390/ijms17101768

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