Dendrimers are efficient drug delivery systems particularly useful in ocular diseases. In particular, low generation PAMAM dendrimers are non-toxic and non-immunogenic and they provide an enhancement of the residence time of drugs in the eyes. In this context, the synthesis of the PAMAM-based matrix metalloproteinases inhibitor 5, is reported. In particular, we demonstrated that 5 strongly binds (18.0 nM ± 2.5 nM) MMP-9, the most relevant MMP responsible of ocular surface damages in induced dry eyes syndrome (DES)
Synthesis and binding monitoring of a new nanomolar PAMAM-based matrix metalloproteinases inhibitor (MMPIs) / Cerofolini, Linda; Baldoneschi, Veronica; Dragoni, Elisa; Storai, Andrea; Mamusa, Marianna; Berti, Debora; Fragai, Marco; Richichi, Barbara; Nativi, Cristina. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 25:(2017), pp. 523-527. [10.1016/j.bmc.2016.11.028]
Synthesis and binding monitoring of a new nanomolar PAMAM-based matrix metalloproteinases inhibitor (MMPIs)
CEROFOLINI, LINDA;BALDONESCHI, VERONICA;DRAGONI, ELISA;BERTI, DEBORA;FRAGAI, MARCO;RICHICHI, BARBARA;NATIVI, CRISTINA
2017
Abstract
Dendrimers are efficient drug delivery systems particularly useful in ocular diseases. In particular, low generation PAMAM dendrimers are non-toxic and non-immunogenic and they provide an enhancement of the residence time of drugs in the eyes. In this context, the synthesis of the PAMAM-based matrix metalloproteinases inhibitor 5, is reported. In particular, we demonstrated that 5 strongly binds (18.0 nM ± 2.5 nM) MMP-9, the most relevant MMP responsible of ocular surface damages in induced dry eyes syndrome (DES)File | Dimensione | Formato | |
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