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Integrin-αvβ3 as a Therapeutic Target in Glioblastoma: Back to the Future?

Département de Biologie Médicale, Centre Scientifique de Monaco, 98000 Monaco, Monaco
Nuclear Medicine Department, Centre Hospitalier Princesse Grace, 98000 Monaco, Monaco
Institute for Research on Cancer and Aging of Nice, Centre Antoine Lacassagne, CNRS UMR 7284, INSERM U1081, Université Cote d’Azur, 06200 Nice, France
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editors: Mohamed Altai and Joanna Strand
Pharmaceutics 2022, 14(5), 1053;
Received: 12 April 2022 / Revised: 4 May 2022 / Accepted: 9 May 2022 / Published: 13 May 2022
(This article belongs to the Special Issue Radionuclide-Based Theranostics)
Glioblastoma (GBM), the most common primary malignant brain tumor, is associated with a dismal prognosis. Standard therapies including maximal surgical resection, radiotherapy, and temozolomide chemotherapy remain poorly efficient. Improving GBM treatment modalities is, therefore, a paramount challenge for researchers and clinicians. GBMs exhibit the hallmark feature of aggressive invasion into the surrounding tissue. Among cell surface receptors involved in this process, members of the integrin family are known to be key actors of GBM invasion. Upregulation of integrins was reported in both tumor and stromal cells, making them a suitable target for innovative therapies targeting integrins in GBM patients, as their impairment disrupts tumor cell proliferation and invasive capacities. Among them, integrin-αvβ3 expression correlates with high-grade GBM. Driven by a plethora of preclinical biological studies, antagonists of αvβ3 rapidly became attractive therapeutic candidates to impair GBM tumorigenesis. In this perspective, the advent of nuclear medicine is currently one of the greatest components of the theranostic concept in both preclinical and clinical research fields. In this review, we provided an overview of αvβ3 expression in GBM to emphasize the therapeutic agents developed. Advanced current and future developments in the theranostic field targeting αvβ3 are finally discussed. View Full-Text
Keywords: glioblastoma; integrins; cilengitide; nuclear medicine; theranostics glioblastoma; integrins; cilengitide; nuclear medicine; theranostics
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MDPI and ACS Style

Echavidre, W.; Picco, V.; Faraggi, M.; Montemagno, C. Integrin-αvβ3 as a Therapeutic Target in Glioblastoma: Back to the Future? Pharmaceutics 2022, 14, 1053.

AMA Style

Echavidre W, Picco V, Faraggi M, Montemagno C. Integrin-αvβ3 as a Therapeutic Target in Glioblastoma: Back to the Future? Pharmaceutics. 2022; 14(5):1053.

Chicago/Turabian Style

Echavidre, William, Vincent Picco, Marc Faraggi, and Christopher Montemagno. 2022. "Integrin-αvβ3 as a Therapeutic Target in Glioblastoma: Back to the Future?" Pharmaceutics 14, no. 5: 1053.

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