Targeting integrin αvβ6 with gallium-68 tris (hydroxypyridinone) based PET probes

Abstract

Expression of the cellular transmembrane receptor αvβ6 integrin is mostly restricted to malignant epithelial cells in a wide variety of carcinomas, including pancreatic and others derived from epithelial tissues. Thus,...

Total Bio-Based Material for Drug Delivery and Iron Chelation to Fight Cancer through Antimicrobial Activity

“…Nanomaterials can be functionalized to actively target tumor tissues or cancer cells and accumulate at tumor sites through surface modification. For instance, cancer-targeting peptides can identify specific receptors [ 16 , 17 , 18 , 19 ], cationic elements can be added to nanomaterials’ surfaces to improve their tumor-penetrating ability [ 20 ], and nanomaterials’ shape or size can be altered to enhance tumor retention. Second, nanomaterials’ distinctive hydrophobic and hydrophilic architectures enable the loading of various medications in relatively high quantities, improving their solubility and safeguarding them against deterioration [ 21 , 22 , 23 ].…”

Peptide-based positron emission tomography probes: current strategies for synthesis and radiolabelling

“…The developed NHS-THP chelator could be used for simple, efficient labelling of 67 Ga/ 68 Ga biomolecules under suitable conditions for peptides and proteins in the aqueous phase and with easy synthetic procedures. In a recent study by Floresta and co-workers 93 , the NHS-THP chemistry was further explored by developing two analogues with two different linkers: bis-NHS-glutaric acid ester and bis-NHS-adipic acid ester. The THP-based compounds were then conjugated to a cyclic peptide that targets the αvβ6 integrin to discover new 68 Ga-labelled radiopharmaceuticals effective for imaging tumours via αvβ6 integrin.…”

“…The developed NHS-THP chelator could be used for simple, efficient labelling of 67 Ga/ 68 Ga biomolecules under suitable conditions for peptides and proteins in the aqueous phase and with easy synthetic procedures. In a recent study by Floresta and co-workers, 93 the NHS-THP chemistry was Scheme 10 Synthetic scheme for THP-succinic (7) and THP-glutaric (8).…”

Beyond transition block metals: exploring the reactivity of phosphine PTA and its oxide [PTA(O)] towards gallium(iii)

“…Among these elements, gallium represents an interesting metal for the development of modern semiconductor materials for the electronic industry 35,36 as well as for the use in medicine to access new diagnostic and therapeutic agents. [37][38][39][40][41] The idea behind the use of gallium in therapy originates from the high similarity between Ga 3+ and Fe 3+ ions, in terms of ionic radius, electronic conguration, coordination number and ligand-donor preferences. 42 Moreover, Ga 3+ and Fe 3+ complexes with organic ligands are oen isostructural.…”