Synthesis and binding monitoring of a new nanomolar PAMAM-based matrix metalloproteinases inhibitor (MMPIs)

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• 作者：Linda Cerofolini^a ; ^b ; ^c ; Veronica Baldoneschi^a ; ^c ; Elisa Dragoni^a ; Andrea Storai^a ; Marianna Mamusa^a ; Debora Berti^a ; Marco Fragai^a ; ^b ; ^{fragai@cerm.unifi.it} ; Barbara Richichi^a ; ^{barbara.richichi@unifi.it} ; Cristina Nativi^a ; ^b
• 关键词：Inhibitors ; Metalloproteins ; Dendrimers ; Sulphonamidic scaffold ; NMR spectroscopy
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：15 January 2017
• 年：2017
• 卷：25
• 期：2
• 页码：523-527
• 全文大小：660 K
• 卷排序：25

文摘

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).