http://www.cnr.it/ontology/cnr/individuo/prodotto/ID212523
Evaluation of the anti-angiogenic properties of the new selective alpha(V)beta(3) integrin antagonist RGDechiHCit (Articolo in rivista)
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- Label
- Evaluation of the anti-angiogenic properties of the new selective alpha(V)beta(3) integrin antagonist RGDechiHCit (Articolo in rivista) (literal)
- Anno
- 2011-01-01T00:00:00+01:00 (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
- 10.1186/1479-5876-9-7 (literal)
- Alternative label
Santulli G., Basilicata MF., De Simone M., Del Giudice C., Anastasio A., Sorriento D., Saviano M., Del Gatto A., Trimarco B., Pedone C., Zaccaro L., Iaccarino G (2011)
Evaluation of the anti-angiogenic properties of the new selective alpha(V)beta(3) integrin antagonist RGDechiHCit
in Journal of translational medicine (Online)
(literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
- Santulli G., Basilicata MF., De Simone M., Del Giudice C., Anastasio A., Sorriento D., Saviano M., Del Gatto A., Trimarco B., Pedone C., Zaccaro L., Iaccarino G (literal)
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- http://www.translational-medicine.com/content/9/1/7 (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
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- Department of Clinical Medicine, Cardiovascular & Immunologic Sciences, \"Federico II\" University of Naples, Italy
Department of Biological Sciences, \"Federico II\" University of Naples, Italy
Institute of Crystallography (Consiglio Nazionale delle Ricerche, CNR), Bari, Italy
Institute of Biostructures and Bioimaging (Consiglio Nazionale delle Ricerche, CNR), Naples, Italy (literal)
- Titolo
- Evaluation of the anti-angiogenic properties of the new selective alpha(V)beta(3) integrin antagonist RGDechiHCit (literal)
- Abstract
- Background
Integrins are heterodimeric receptors that play a critical role in cell-cell and cell-matrix adhesion processes. Among them, ?V?3 integrin, that recognizes the aminoacidic RGD triad, is reported to be involved in angiogenesis, tissue repair and tumor growth. We have recently synthesized a new and selective ligand of ?V?3 receptor, referred to as RGDechiHCit, that contains a cyclic RGD motif and two echistatin moieties.
Methods
The aim of this study is to evaluate in vitro and in vivo the effects of RGDechiHCit. Therefore, we assessed its properties in cellular (endothelial cells [EC], and vascular smooth muscle cells [VSMC]) and animal models (Wistar Kyoto rats and c57Bl/6 mice) of angiogenesis.
Results
In EC, but not VSMC, RGDechiHCit inhibits intracellular mitogenic signaling and cell proliferation. Furthermore, RGDechiHCit blocks the ability of EC to form tubes on Matrigel. In vivo, wound healing is delayed in presence of RGDechiHCit. Similarly, Matrigel plugs demonstrate an antiangiogenic effect of RGDechiHCit.
Conclusions
Our data indicate the importance of RGDechiHCit in the selective inhibition of endothelial ?V?3 integrin in vitro and in vivo. Such inhibition opens new fields of investigation on the mechanisms of angiogenesis, offering clinical implications for treatment of pathophysiological conditions such as cancer, proliferative retinopathy and inflammatory disease. (literal)
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