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Identification of Novel CK2 Kinase Substrates Using a Versatile Biochemical Approach
Published on: February 21, 2019
Intracellular protein kinase CK2 inhibition by ferulic acid-based trimodal nanodevice
Sofia Zanin1, Simone Molinari2, Giorgio Cozza3
1Department of Molecular Medicine, University of Pavia, via Forlanini 6, 27100 Pavia, Italy.
Abstract:
Protein kinase CK2, a pleiotropic and constitutively active kinase, is strictly involved in different diseases, especially in cancer. Many efforts have been carried out to develop specific CK2 inhibitors and recently, it has been evidenced that ferulic acid (FA) represents a promising, albeit cell impermeable, CK2 inhibitor. In the present study, the potential of a nanotechnological approach to cope with intracellular CK2 regulation was explored. Surface-Active Maghemite Nanoparticles (SAMNs), coupling magnetism with photoluminescence, a new feature of SAMNs here described for the first time, were chosen as dual imaging nanocarrier for FA. The self-assembled nanodevice (SAMN@FA) displayed a significant CK2 inhibitory activity in vitro. Moreover, effective cellular internalization of SAMN@FA in cancer cells was proved by direct visualization of the photoluminescent nanocarrier by confocal microscopy and was corroborated by phosphorylation levels of endogenous CK2 targets. The proposed trimodal nanodevice, representing the first example of cellular CK2 nano-inhibition, paves the way for novel active nanocarriers as appealing theranostic tool for future biomedical applications.
Insights
Ferulic acid (FA), a CK2 inhibitor, was encapsulated in novel magnetic nanoparticles (SAMNs) for cancer therapy. This nanocarrier (SAMN@FA) effectively delivered FA into cancer cells, inhibiting CK2 activity and offering a new theranostic tool.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Molecular Biology
Background:
- Protein kinase CK2 is a key target in cancer therapy.
- Ferulic acid (FA) shows promise as a CK2 inhibitor but has poor cell permeability.
- Nanotechnology offers potential solutions for targeted drug delivery.
Purpose of the Study:
- To develop a nanocarrier for intracellular delivery of ferulic acid (FA) to inhibit CK2.
- To explore the theranostic potential of Surface-Active Maghemite Nanoparticles (SAMNs) loaded with FA (SAMN@FA).
Main Methods:
- Surface-Active Maghemite Nanoparticles (SAMNs) were synthesized and characterized.
- FA was loaded onto SAMNs to create the SAMN@FA nanodevice.
- In vitro CK2 inhibition assays and cellular uptake studies using confocal microscopy were performed in cancer cells.
Main Results:
- The SAMN@FA nanodevice demonstrated significant in vitro CK2 inhibitory activity.
- Confocal microscopy confirmed efficient cellular internalization of SAMN@FA in cancer cells.
- Inhibition of CK2 targets' phosphorylation levels corroborated the nanodevice's efficacy.
Conclusions:
- This study presents the first example of cellular CK2 nano-inhibition using a trimodal nanodevice.
- SAMN@FA is a promising theranostic tool for cancer treatment, enabling targeted delivery and imaging.
- This nanotechnological approach overcomes FA's cell permeability limitations for effective CK2 inhibition.
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