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Targeting G Protein‐Coupled Receptors with Magnetic Carbon Nanotubes: The Case of the A 3 Adenosine Receptor
Author(s) -
Pineux Florent,
Federico Stephanie,
Klotz KarlNorbert,
Kachler Sonja,
Michiels Carine,
Sturlese Mattia,
Prato Maurizio,
Spalluto Giampiero,
Moro Stefano,
Bonifazi Davide
Publication year - 2020
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202000466
Subject(s) - linker , receptor , g protein coupled receptor , adenosine receptor , ligand (biochemistry) , cancer cell , biophysics , chemistry , docking (animal) , radioligand , nanotechnology , cell , biochemistry , materials science , cancer , biology , medicine , computer science , nursing , genetics , agonist , operating system
The A 3 adenosine receptor (AR) is a G protein‐coupled receptor (GPCR) overexpressed in the membrane of specific cancer cells. Thus, the development of nanosystems targeting this receptor could be a strategy to both treat and diagnose cancer. Iron‐filled carbon nanotubes (CNTs) are an optimal platform for theranostic purposes, and the use of a magnetic field can be exploited for cancer magnetic cell sorting and thermal therapy. In this work, we have conjugated an A 3 AR ligand on the surface of iron‐filled CNTs with the aim of targeting cells overexpressing A 3 ARs. In particular, two conjugates bearing PEG linkers of different length were designed. A docking analysis of A 3 AR showed that neither CNT nor linker interferes with ligand binding to the receptor; this was confirmed by in vitro preliminary radioligand competition assays on A 3 AR. Encouraged by this result, magnetic cell sorting was applied to a mixture of cells overexpressing or not the A 3 AR in which our compound displayed indiscriminate binding to all cells. Despite this, it is the first time that a GPCR ligand has been anchored to a magnetic nanosystem, thus it opens the door to new applications for cancer treatment.

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