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Open AccessArticle

Bone-Seeking Matrix Metalloproteinase Inhibitors for the Treatment of Skeletal Malignancy

1
Department of Pharmacy and Pharmaceutical Sciences, University of Bari “A. Moro”, via E. Orabona 4, 70125 Bari, Italy
2
Department of Pharmacy, University “G. d’Annunzio” of Chieti-Pescara, Via Dei Vestini, 31, 66100 Chieti, Italy
3
Leibniz-Institute for Food Systems Biology at the Technical University of Munich, Lise-Meitner-Str. 34, 85354 Freising, Germany
4
Istituto di Cristallografia, Consiglio Nazionale delle Ricerche, Montelibretti, Monterotondo Stazione, 00015 Roma, Italy
5
Tumor Biology Department, H. Lee Moffitt Cancer Center and Research Institute, Tampa, FL 33612, USA
*
Authors to whom correspondence should be addressed.
Pharmaceuticals 2020, 13(6), 113; https://doi.org/10.3390/ph13060113
Received: 9 May 2020 / Revised: 29 May 2020 / Accepted: 30 May 2020 / Published: 1 June 2020
(This article belongs to the Section Pharmacology)
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. View Full-Text
Keywords: bisphosphonates; matrix metalloproteinase inhibitors; antitumor agent; bone targeting; skeletal malignancies bisphosphonates; matrix metalloproteinase inhibitors; antitumor agent; bone targeting; skeletal malignancies
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MDPI and ACS Style

Laghezza, A.; Piemontese, L.; Brunetti, L.; Caradonna, A.; Agamennone, M.; Di Pizio, A.; Pochetti, G.; Montanari, R.; Capelli, D.; Tauro, M.; Loiodice, F.; Tortorella, P. Bone-Seeking Matrix Metalloproteinase Inhibitors for the Treatment of Skeletal Malignancy. Pharmaceuticals 2020, 13, 113.

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