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

Floresta, Giuseppe; Memdouh, Siham; Pham, Truc Thuy; Michelle, T.; Blower, Philip J.; Hider, Robert C.; Abbate, Vincenzo; Cilibrizzi, Agostino

doi:10.1039/d2dt00980c

Cited by 5 publications

(4 citation statements)

References 34 publications

(71 reference statements)

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“…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 ].…”

Section: Introductionmentioning

confidence: 99%

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

et al. 2023

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Bacterial involvement in cancer’s development, along with their impact on therapeutic interventions, has been increasingly recognized. This has prompted the development of novel strategies to disrupt essential biological processes in microbial cells. Among these approaches, metal-chelating agents have gained attention for their ability to hinder microbial metal metabolism and impede critical reactions. Nanotechnology has also contributed to the antibacterial field by offering various nanomaterials, including antimicrobial nanoparticles with potential therapeutic and drug-delivery applications. Halloysite nanotubes (HNTs) are naturally occurring tubular clay nanomaterials composed of aluminosilicate kaolin sheets rolled multiple times. The aluminum and siloxane groups on the surface of HNTs enable hydrogen bonding with biomaterials, making them versatile in various domains, such as environmental sciences, wastewater treatment, nanoelectronics, catalytic studies, and cosmetics. This study aimed to create an antibacterial material by combining the unique properties of halloysite nanotubes with the iron-chelating capability of kojic acid. A nucleophilic substitution reaction involving the hydroxyl groups on the nanotubes’ surface was employed to functionalize the material using kojic acid. The resulting material was characterized using infrared spectroscopy (IR), thermogravimetric analysis (TGA), energy-dispersive X-ray spectroscopy (EDX), and scanning electron microscopy (SEM), and its iron-chelating ability was assessed. Furthermore, the potential for drug loading—specifically, with resveratrol and curcumin—was evaluated through ultraviolet (UV) analysis. The antibacterial assay was evaluated following CLSI guidelines. The results suggested that the HNTs–kojic acid formulation had great antibacterial activity against all tested pathogens. The outcome of this work yielded a novel bio-based material with dual functionality as a drug carrier and an antimicrobial agent. This innovative approach holds promise for addressing challenges related to bacterial infections, antibiotic resistance, and the development of advanced therapeutic interventions.

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Section: Introductionmentioning

confidence: 99%

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

et al. 2023

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“…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.…”

Section: Rsc Medicinal Chemistry Accepted Manuscriptmentioning

confidence: 99%

Section: Rsc Medicinal Chemistry Reviewmentioning

confidence: 99%

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

2023

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“…This field of application is particularly relevant because of the rising global frequency of malignant tumors in the population. The interactions of the radiolabeled peptide-based probe with cancer cells are typically carried out through protein structures that are overexpressed in these malignant cells [ 14 , 15 , 16 , 17 , 18 , 19 ]. These radioactive isotopes can be attached to peptides to create imaging probes that bind to specific molecular targets in vivo.…”

Section: Introductionmentioning

confidence: 99%

Computer-Assisted Design of Peptide-Based Radiotracers

Patamia

Zagni

Brullo

et al. 2023

IJMS

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In medical imaging, techniques such as magnetic resonance imaging, contrast-enhanced computerized tomography, positron emission tomography (PET), and single-photon emission computed tomography (SPECT) are extensively available and routinely used for disease diagnosis. PET probes with peptide-based targeting are typically composed of small peptides especially developed to have high affinity and specificity for a range of cellular and tissue targets. These probes’ key benefits include being less expensive than traditional antibody-based PET tracers and having an effective chemical modification process that allows them to be radiolabeled with almost any radionuclide, making them highly appealing for clinical usage. Currently, as with every pharmaceutical design, the use of in silico strategies is steadily growing in this field, even though it is not part of the standard toolkit used during radiopharmaceutical design. This review describes the recent applications of computational design approaches in the design of novel peptide-based radiopharmaceuticals.

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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,...

Cited by 5 publications

References 34 publications

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

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

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

Computer-Assisted Design of Peptide-Based Radiotracers

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