Increasing αvβ3 Selectivity of the Anti-Angiogenic Drug Cilengitide by N-Methylation
| Autor: | Sandro Cosconati, Lucas Doedens, Andreas O. Frank, Ettore Novellino, Luciana Marinelli, Johannes G. Beck, Horst Kessler, Carlos Mas-Moruno |
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| Přispěvatelé: | Mas Moruno, C, Beck, Jg, Doedens, L, Frank, Ao, Marinelli, L, Cosconati, Sandro, Novellino, E, Kessler, H., Mas Moruno, C., Beck, J. G., Doedens, L., Frank, A. O., Marinelli, Luciana, Cosconati, S., Novellino, Ettore, Universitat Politècnica de Catalunya. Departament de Ciència dels Materials i Enginyeria Metal·lúrgica |
| Rok vydání: | 2011 |
| Předmět: |
Protein Conformation
integrin education Integrin Angiogenesis Inhibitors Cilengitide Molecular Dynamics Simulation Enginyeria dels materials [Àrees temàtiques de la UPC] Methylation Peptides Cyclic Catalysis cyclic peptide Structure-Activity Relationship chemistry.chemical_compound Protein structure Peptide Library Structure–activity relationship Peptide bond Receptors Vitronectin Drugs--Design skin and connective tissue diseases Peptide library Nuclear Magnetic Resonance Biomolecular Medicaments -- Disseny biology Chemistry receptor selectivity cyclic peptides General Chemistry N-methylation Integrin alphaVbeta3 Biochemistry conformational studie Cancer research biology.protein conformational studies sense organs Selectivity psychological phenomena and processes Snake Venoms |
| Zdroj: | UPCommons. Portal del coneixement obert de la UPC Universitat Politècnica de Catalunya (UPC) Recercat. Dipósit de la Recerca de Catalunya Universitat Jaume I |
| ISSN: | 1433-7851 |
| DOI: | 10.1002/anie.201102971 |
| Popis: | Thumbnail image of graphical abstract A subtle change: Structural changes upon amide bond methylation improve the selectivity of the anti-angiogenic drug Cilengitide, which after N-methylation at distinct positions discriminates between the closely related pro-angiogenic integrins avß3 and avß5 (see scheme). |
| Databáze: | OpenAIRE |
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