A stapled chromogranin A-derived peptide is a potent dual ligand for integrins αvβ6 and αvβ8

Combining 2D STD-NMR, computation, biochemical assays and click-chemistry, we have identified a chromogranin-A derived compound ( 5 ) that has high affinity and bi-selectivity for αvβ6 and αvβ8 integrins and is stable in microsomal preparations. 5 is suitable for nanoparticle functionalization and d...

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Veröffentlicht in:	Chemical communications (Cambridge, England) England), 2019-12, Vol.55 (98), p.14777-1478
Hauptverfasser:	Nardelli, Francesca, Ghitti, Michela, Quilici, Giacomo, Gori, Alessandro, Luo, Qingqiong, Berardi, Andrea, Sacchi, Angelina, Monieri, Matteo, Bergamaschi, Greta, Bermel, Wolfgang, Chen, Fuxiang, Corti, Angelo, Curnis, Flavio, Musco, Giovanna
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Antigens, Neoplasm - metabolism Cell Line, Tumor Chromogranin A - chemistry Diagnostic software Diagnostic systems Humans Integrins - antagonists & inhibitors Integrins - metabolism Ligands Microscopy, Fluorescence Nanoparticles NMR Nuclear magnetic resonance Nuclear Magnetic Resonance, Biomolecular Organic chemistry Peptides - chemistry Peptides - metabolism Protein Binding Selectivity
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Zusammenfassung:	Combining 2D STD-NMR, computation, biochemical assays and click-chemistry, we have identified a chromogranin-A derived compound ( 5 ) that has high affinity and bi-selectivity for αvβ6 and αvβ8 integrins and is stable in microsomal preparations. 5 is suitable for nanoparticle functionalization and delivery to cancer cells, holding promise for diagnostic and/or therapeutic applications. Combining 2D STD-NMR, computation, biochemical assays and click-chemistry, we have identified a chromogranin-A derived compound ( 5 ) that has high affinity and bi-selectivity for αvβ6 and αvβ8 integrins and is stable in microsomal preparations.
ISSN:	1359-7345 1364-548X
DOI:	10.1039/c9cc08518a