Surface-functionalized gold nanoparticles (AuNPs) are being developed as cancer therapeutics and imaging agents to target affected cells/organs and by minimizing the side effects. G protein-coupled receptors (GPCRs) belong to a superfamily of cell surface signaling receptors having important roles in many physiological functions and disease states. The four subtypes of adenosine (ARs) receptors, A1, A2A, A2B and A3, are GPCRs with therapeutic potential for a wide range of diseases including cancer.We have tethered to the functionalized gold surface specific ligands, agonists and antagonists, of ARs, as models for cell surface GPCRs, and found retention of the biological properties. These adenosine ligands conjugated AuNPs were in average diameters of 2-4.5 nm range and showed excellent water solubility. Pharmacological studies on these AuNP conjugates were performed in mammalian cells expressing CHO cells (A1 and A3) or HEK293 cells (A2A) stably expressing a hAR subtype. This is the first prototypical application to gold carriers of small molecule GPCR ligands that are under investigation for treatment of cancer and inflammatory diseases.

Design of adenosine receptor agonist- and antagonist-conjugated gold nanoparticles for therapeutic applications including cancer

244th National Meeting (2012)

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