Events MOL2NET'16, Conference on Molecular, Biomed., Comput. & Network Science and Engineering, 2nd ed.

Event submissions

Published

This submission belongs to the session 02. CHEMBIOMOL-02: Chem. Biol. & Med. Chem. Workshop, Rostock, Germany-Bilbao, Spain-Galveston, Texas, USA, 2016 of the event MOL2NET'16, Conference on Molecular, Biomed., Comput. & Network Science and Engineering, 2nd ed.

Published date

12 Oct, 2016

Citation

Nerea Zabala Uncilla, Claudio Palomo Nicolau, Jose Ignacio Gamboa Landa, Jose Luis Castrillo, Silvia Avila, Depsipeptides and peptide-mimetics, cyclics and acyclics, integrin αVβ₃ inhibitors., in Proceedings of MOL2NET'16, Conference on Molecular, Biomed., Comput. & Network Science and Engineering, 2nd ed., 15 October–20 October 2022, MDPI: Basel, Switzerland, doi: 10.3390/mol2net-02-08012

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Depsipeptides and peptide-mimetics, cyclics and acyclics, integrin α_Vβ₃ inhibitors.

Nerea Zabala Uncilla ¹

Claudio Palomo Nicolau ²

Jose Ignacio Gamboa Landa ²

Jose Luis Castrillo ³

Silvia Avila ²

1. Department of Organic Chemistry II, University of the Basque Country UPV/EHU, 48940, Bilbao, Spain.

2. Departamento de Química Orgánica I, Facultad de Química, Universidad del País Vasco, Manuel Lardizabal 3, 20018 Donostia, Spain

3. GENETADI Biotech, Parque Teconologico 502 Derio-BILBAO (SPAIN) 48160 Spain

Abstract

Angiogenesis, the sprouting of new blood vessels from pre-existing vessels, is a remarkable feature of tumours growth and metastasis. The in vivo inhibition of this receptor by cyclic peptides containing RGD sequence may be used to selectively suppress these disease¹. Our research group has developed a new methodology² for the evaluation of new antiangiogenic compounds, based in the genetic expression analysis using CGH array system. The RGD mimetics activity can be modified by the presence of ester-bond³, Therefore, we decided to prepare some depsipeptides analogous to the RGD-β-lactam compounds and evaluate their activity performing a genetic expression analysis. We also have evaluated the activity of open-chain compounds without RGD formal structure. The cyclic depsipeptides have demonstrated a very effective inhibitory activity. In the other hand the open-chain compounds have a surprising behavior, demonstrating a similar gene activation. This way, we call into question the essential need of RGD sequence to have an interaction between ligand and the receptor of the integrin^{4, 5}.

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Keywords

Desipeptides

Peptide-mimetics

Integrin inhibitors

Poster

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