ArticleInternational journal of oncology2013
A small-molecule RGD-integrin antagonist inhibits cell adhesion, cell migration and induces anoikis in glioblastoma cells.
Article in International journal of oncology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.
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Who cites it
40 citing papers in PubMed, 84 citations in OpenAlex.
- Extracellular Matrix Microstructures Directly Regulate Glutathione Bioavailability in Human Hepatocytes.Biomacromolecules · 2025Article
- Extracellular Matrix Microstructures Modulate Hepatic Methionine Cycle and Methylations.Biomacromolecules · 2025Article
- Inhibiting fibronectin assembly in the breast tumor microenvironment increases cell death and improves response to doxorubicin.bioRxiv : the preprint server for biology · 2025Article
- RGD peptide promotes follicle growth through integrins αvβ3/αvβ5 in three-dimensional culture.Reproduction (Cambridge, England) · 2025Article
- Extracellular Vesicle Mobility in Collagen I Hydrogels Is Influenced by Matrix-Binding Integrins.ACS nano · 2024Article
- Family-Wide Photoproximity Profiling of Integrin Protein Social Networks in Cancer.bioRxiv : the preprint server for biology · 2024Article
- Forms of Non-Apoptotic Cell Death and Their Role in Gliomas-Presentation of the Current State of Knowledge.Biomedicines · 2024Review
- Enhancing Viability of Human Embryonic Stem Cells during Cryopreservation via RGD-REP-Mediated Activation of FAK/AKT/FoxO3a Signaling Pathway.Tissue engineering and regenerative medicine · 2023Article
- The Prognosis of Cancer Depends on the Interplay of Autophagy, Apoptosis, and Anoikis within the Tumor Microenvironment.Cell biochemistry and biophysics · 2023Review
- Tumor Niches: Perspectives for Targeted Therapies in Glioblastoma.Antioxidants & redox signaling · 2023Review
- Circulating Tumor Cells Adhesion: Application in Biosensors.Biosensors · 2023Review
- Article
- Bioinformatics based exploration of hsa-miR-194-5p regulation of CHD4 through PI3K/AKT signal pathway to enhance tumor resistance to apoptosis due to loss of nests and participate in poor prognosis of oral squamous cell carcinoma.Annals of translational medicine · 2023Article
- Nintedanib-αVβ6 Integrin Ligand Conjugates Reduce TGFInternational journal of molecular sciences · 2023Article
- Broad spectrum integrin inhibitor GLPG-0187 bypasses immune evasion in colorectal cancer by TGF-β signaling mediated downregulation of PD-L1.American journal of cancer research · 2023Article
- Anoikis resistance in diffuse glioma: The potential therapeutic targets in the future.Frontiers in oncology · 2022Review
- Pathophysiological roles of integrins in gliomas from the perspective of glioma stem cells.Frontiers in cell and developmental biology · 2022Review
- Anti-Cancer Effects of Cyclic Peptide ALOS4 in a Human Melanoma Mouse Model.International journal of molecular sciences · 2021Article
- Nanoformulation Shows Cytotoxicity against Glioblastoma Cell Lines and Antiangiogenic Activity in Chicken Chorioallantoic Membrane.Pharmaceutics · 2021Article
- Review
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In cancer cells integrins modulate important cellular events that regulate the metastasic cascade which involves detachment from the tumor mass, dissemination and attachment to the oncogenic niche. The α5β1, αvβ3 and αvβ5 integrins are widely expressed in different cancer types and recognize the tripeptide Arg-Gly-Asp (RGD) motif present in several extracellular matrix proteins. In human glioblastoma, αvβ3 integrin expression correlates with tumor grade, suggesting that this integrin may play a crucial role in the highly infiltrative behavior of high grade gliomas. However, few selective RGD-like antagonists have been developed and few studies have investigated their effects in in vitro models of human glioblastoma. In this study, we investigated several cellular effects and the underlying molecular mechanisms exerted by a new small-molecule RGD antagonist, 1a-RGD, in the U251 and U373 human glioblastoma cell lines. Treatment with 1a-RGD (20 µM) demonstrated a weak effect on cell viability and cell proliferation but strongly inhibited cell attachment and cell migration together with actin cytoskeleton disassembly. Prolonged 1a-RGD treatment (72 h) induced anoikis, assessed by Annexin staining and nucleosome assay, particularly in the detached cells. When integrin-linked transduction pathways were investigated, 1aRGD was found to exert a marked reduction in focal adhesion kinase (FAK) phosphorylation without affecting the AKT- and ERK-dependent pathways. Our data indicate that 1a-RGD, probably via modulation of the FAK-dependent pathway, inhibits cell migration and attachment and induces anoikis in glioblastoma cells. This novel finding suggests that the development of an RGD-like molecule may represent a promising tool for the pharmacological approach aimed at reducing the malignancy of glioblastoma cells.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.