Bone-seeking matrix metalloproteinase inhibitors for the treatment of skeletal malignancy

Antonio Laghezza, Luca Piemontese, Leonardo Brunetti, Alessia Caradonna, Mariangela Agamennone, Antonella Di Pizio, Giorgio Pochetti, Roberta Montanari, Davide Capelli, Marilena Tauro, Fulvio Loiodice, Paolo Tortorella

Research output: Contribution to journalArticlepeer-review

3 Scopus citations


Matrix metalloproteinases (MMPs) are a family of enzymes involved at different stages of cancer progression and metastasis. We previously identified a novel class of bisphosphonic inhibitors, selective for MMPs crucial for bone remodeling, such as MMP-2. Due to the increasing relevance of specific MMPs at various stages of tumor malignancy, we focused on improving potency towards certain isoforms. Here, we tackled MMP-9 because of its confirmed role in tumor invasion, metastasis, angiogenesis, and immuno-response, making it an ideal target for cancer therapy. Using a computational analysis, we designed and characterized potent MMP-2/MMP-9 inhibitors. This is a promising approach to develop and clinically translate inhibitors that could be used in combination with standard care therapy for the treatment of skeletal malignancies.

Original languageEnglish
Article number113
Issue number6
StatePublished - 2020
Externally publishedYes


  • Antitumor agent
  • Bisphosphonates
  • Bone targeting
  • Matrix metalloproteinase inhibitors
  • Skeletal malignancies


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