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Pharmacophoric modifications lead to superpotent avß3 integrin ligands with suppressed a5ß1 activity
Neubauer, Stefanie; Rechenmacher, Florian; Brimioulle, Richard; Di Leva, Francisco Saverio; Bochen, Alexander; Sobahi, Tariq R.; Schottelius, Margret; Novellino, Ettore; Mas Moruno, Carlos; Marinelli, Luciana; Kessler, Horst
Universitat Politècnica de Catalunya. Departament de Ciència dels Materials i Enginyeria Metal·lúrgica; Universitat Politècnica de Catalunya. BIBITE - Biomaterials, Biomecànica i Enginyeria de Teixits
The selective targeting of the avß3 integrin subtype without affecting the structurally closely related receptor a5ß1 is crucial for understanding the details of their biological and pathological functions and thus of great relevance for diagnostic and therapeutic approaches in cancer treatment. Here, we present the synthesis of highly active RGD peptidomimetics for the avß3 integrin with remarkable selectivity against a5ß1. Incorporation of a methoxypyridine building block into a ligand scaffold and variation of different functional moieties led to avß3-antagonistic activities in the low nanomolar or even subnanomolar range. Furthermore, docking studies were performed to give insights into the binding modes of the novel compounds. The presented library comprises powerful ligands for specific addressing and blocking of the avß3 integrin subtype, thereby representing privileged tools for integrin-based personalized medicine
Peer Reviewed
Àrees temàtiques de la UPC::Enginyeria dels materials
Càncer -- Teràpia
Pèptids -- Síntesi
Attribution-NonCommercial-NoDerivs 3.0 Spain

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