Impact of Selected Small-Molecule Kinase Inhibitors on Lipid Membranes
Abstract
:1. Introduction
2. Results
2.1. Localization of Kinase Inhibitors in the Membrane
2.2. Influence of Kinase Inhibitors on Headgroup and Acyl Chain Behavior of the Phospholipid Membrane
2.3. Influence of Kinase Inhibitors on Transmembrane Permeation of Anions
2.4. Influence of Kinase Inhibitors on Fluorescence Lifetime of NBD Labelled Vesicles
3. Discussion
4. Materials and Methods
4.1. Chemicals
4.2. Preparation of LUVs
4.3. Sample Preparation for NMR Experiments
4.4. H NMR and 31P NMR Spectroscopy
4.5. H MAS NMR Spectroscopy
4.6. Measurement of Membrane Permeation of Polar Molecules
4.7. Measurement of Fluorescence Lifetime
Supplementary Materials
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
References
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31P CSA (ppm) | Lc*[Å] | <S> | |
---|---|---|---|
POPC | 45 | 11.0 | 0.144 |
+Erlotinib | 45 | 11.6 | 0.154 |
+Lenvatinib | 44 | 11.2 | 0.147 |
+Sunitinib | 47 | 10.6 | 0.130 |
+Idelalisib | 44 | 10.8 | 0.136 |
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Luck, M.; Fischer, M.; Werle, M.; Scheidt, H.A.; Müller, P. Impact of Selected Small-Molecule Kinase Inhibitors on Lipid Membranes. Pharmaceuticals 2021, 14, 746. https://doi.org/10.3390/ph14080746
Luck M, Fischer M, Werle M, Scheidt HA, Müller P. Impact of Selected Small-Molecule Kinase Inhibitors on Lipid Membranes. Pharmaceuticals. 2021; 14(8):746. https://doi.org/10.3390/ph14080746
Chicago/Turabian StyleLuck, Meike, Markus Fischer, Maximilian Werle, Holger A. Scheidt, and Peter Müller. 2021. "Impact of Selected Small-Molecule Kinase Inhibitors on Lipid Membranes" Pharmaceuticals 14, no. 8: 746. https://doi.org/10.3390/ph14080746