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Targeting Matrix Metalloproteinases: Design of a Bifunctional Inhibitor for Presentation by Tumour-Associated Galectins

Authors

  • Dr. Marco Bartoloni,

    1. Department of Chemistry, University of Florence, Via della Lastruccia, 13 50019 Sesto F.no Firenze (Italy)
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  • Dr. Blanca E. Domínguez,

    1. Centro de Investigationes Biològicas, CSIC, Ramiro de Maetzu 9, 28040 Madrid (Spain)
    2. Centro de Investigaciones Químicas, Universidad Autónoma del Estado de Morelos, Av. Universidad 1001, 62210, Cuernavaca, Morelos (México)
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  • Dr. Elisa Dragoni,

    1. Department of Chemistry, University of Florence, Via della Lastruccia, 13 50019 Sesto F.no Firenze (Italy)
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  • Dr. Barbara Richichi,

    1. Department of Chemistry, University of Florence, Via della Lastruccia, 13 50019 Sesto F.no Firenze (Italy)
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  • Dr. Marco Fragai,

    1. Department of Chemistry, University of Florence, Via della Lastruccia, 13 50019 Sesto F.no Firenze (Italy)
    2. CERM, University of Florence, Via Sacconi, 6 50019 Sesto F.no Firenze (Italy)
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  • Dr. Sabine André,

    1. Institute of Physiological Chemistry, Faculty of Veterinary Medicine, Ludwig-Maximilians-University, Veterinärstr. 13, 80539 München (Germany)
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  • Prof. Hans-Joachim Gabius,

    1. Institute of Physiological Chemistry, Faculty of Veterinary Medicine, Ludwig-Maximilians-University, Veterinärstr. 13, 80539 München (Germany)
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  • Dr. Ana Ardá,

    1. Centro de Investigationes Biològicas, CSIC, Ramiro de Maetzu 9, 28040 Madrid (Spain)
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  • Prof. Claudio Luchinat,

    1. Department of Chemistry, University of Florence, Via della Lastruccia, 13 50019 Sesto F.no Firenze (Italy)
    2. CERM, University of Florence, Via Sacconi, 6 50019 Sesto F.no Firenze (Italy)
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  • Prof. Jesús Jiménez-Barbero,

    Corresponding author
    1. Centro de Investigationes Biològicas, CSIC, Ramiro de Maetzu 9, 28040 Madrid (Spain)
    • Centro de Investigationes Biològicas, CSIC, Ramiro de Maetzu 9, 28040 Madrid (Spain)
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  • Prof. Cristina Nativi

    Corresponding author
    1. Department of Chemistry, University of Florence, Via della Lastruccia, 13 50019 Sesto F.no Firenze (Italy)
    2. CERM, University of Florence, Via Sacconi, 6 50019 Sesto F.no Firenze (Italy)
    • Department of Chemistry, University of Florence, Via della Lastruccia, 13 50019 Sesto F.no Firenze (Italy)
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Abstract

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A new strategy to exploit galectin presence to target matrix metalloproteinases (MMPs) is presented. A bifunctional conjugate with lactose and an inhibitor for MMPs is able to bind MMP and Gal-3 simultaneously. This compound might allow the lectin to attract the MMP inhibitor to the tumour site and to block protumoural activities of the lectin at the same time.

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