Photoactivatable Caged Prodrugs of VEGFR-2 Kinase Inhibitors
AbstractIn this study, we report on the design, synthesis, photokinetic properties and in vitro evaluation of photoactivatable caged prodrugs for the receptor tyrosine kinase VEGFR-2. Highly potent VEGFR-2 inhibitors 1 and 3 were caged by introduction of a photoremovable protecting group (PPG) to yield the caged prodrugs 4 and 5. As expected, enzymatic and cellular proliferation assays showed dramatically diminished efficacy of caged prodrugs in vitro. Upon ultraviolet (UV) irradiation of the prodrugs original inhibitory activity was completely restored and even distinctly reinforced, as was the case for the prodrug 4. The presented results are a further evidence for caging technique being an interesting approach in the protein kinase field. It could enable spatial and temporal control for the inhibition of VEGFR-2. The described photoactivatable prodrugs might be highly useful as biological probes for studying the VEGFR-2 signal transduction. View Full-Text
- Supplementary File 1:
Supplementary (PDF, 789 KB)
Scifeed alert for new publicationsNever miss any articles matching your research from any publisher
- Get alerts for new papers matching your research
- Find out the new papers from selected authors
- Updated daily for 49'000+ journals and 6000+ publishers
- Define your Scifeed now
Pinchuk, B.; Horbert, R.; Döbber, A.; Kuhl, L.; Peifer, C. Photoactivatable Caged Prodrugs of VEGFR-2 Kinase Inhibitors. Molecules 2016, 21, 570.
Pinchuk B, Horbert R, Döbber A, Kuhl L, Peifer C. Photoactivatable Caged Prodrugs of VEGFR-2 Kinase Inhibitors. Molecules. 2016; 21(5):570.Chicago/Turabian Style
Pinchuk, Boris; Horbert, Rebecca; Döbber, Alexander; Kuhl, Lydia; Peifer, Christian. 2016. "Photoactivatable Caged Prodrugs of VEGFR-2 Kinase Inhibitors." Molecules 21, no. 5: 570.
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.