Design, modelling, synthesis and biological evaluation of peptidomimetic phosphinates as inhibitors of matrix metalloproteinases MMP-2 and MMP-8 |
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| Authors: | Bianchini Gianluca Aschi Massimiliano Cavicchio Giancarlo Crucianelli Marcello Preziuso Serena Gallina Carlo Nastari Adele Gavuzzo Enrico Mazza Fernando |
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| Affiliation: | Dipartimento di Chimica, Ingegneria Chimica e Materiali, Università dell'Aquila, via Vetoio, I-67010-Coppito, AQ, Italy. |
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| Abstract: | Three novel peptidomimetic phosphinate inhibitors have been synthesized and evaluated as inhibitors of matrix metalloproteinases MMP-2 and MMP-8. Their IC50 values are in the micromolar range, and one of them showed to be the most effective inhibitor of MMP-2. The differences in binding affinities for MMP-2 and MMP-8 of the three phosphinates have been rationalized by means of modelling studies and molecular dynamics simulations. |
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