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Updated: Aug 31, 2025
Fluorescence-quenching of a Liposomal-encapsulated Near-infrared Fluorophore as a Tool for In Vivo Optical Imaging
Published on: January 5, 2015
Intrinsically Fluorescent Anti-Cancer Drugs
Md Lutful Kabir1, Feng Wang2, Andrew H A Clayton1
1Optical Sciences Centre, Department of Physics and Astronomy, School of Science, Computing and Engineering Technologies, Swinburne University of Technology, Melbourne, VIC 3122, Australia.
Abstract:
At present, about one-third of the total protein targets in the pharmaceutical research sector are kinase-based. While kinases have been attractive targets to combat many diseases, including cancer, selective kinase inhibition has been challenging, because of the high degree of structural homology in the active site where many kinase inhibitors bind. Despite efficacy as cancer drugs, kinase inhibitors can exhibit limited target specificity and rationalizing their target profiles in the context of precise molecular mechanisms or rearrangements is a major challenge for the field. Spectroscopic approaches such as infrared, Raman, NMR and fluorescence have the potential to provide significant insights into drug-target and drug-non-target interactions because of sensitivity to molecular environment. This review places a spotlight on the significance of fluorescence for extracting information related to structural properties, discovery of hidden conformers in solution and in target-bound state, binding properties (e.g., location of binding sites, hydrogen-bonding, hydrophobicity), kinetics as well as dynamics of kinase inhibitors. It is concluded that the information gleaned from an understanding of the intrinsic fluorescence from these classes of drugs may aid in the development of future drugs with improved side-effects and less disease resistance.
Insights
Fluorescence spectroscopy offers valuable insights into kinase inhibitor interactions, aiding in the development of more selective drugs. Understanding drug-target binding properties can lead to improved cancer therapies with fewer side effects.
Area of Science:
- Biochemistry and Molecular Biology
- Pharmacology
- Spectroscopy
Background:
- Kinase-based targets represent a significant portion of pharmaceutical research, particularly for cancer treatment.
- Selective kinase inhibition is difficult due to structural similarities in active sites, leading to challenges in drug specificity.
- Current kinase inhibitors, while effective, often have limited target specificity, complicating mechanistic understanding.
Purpose of the Study:
- To review the utility of fluorescence spectroscopy in characterizing kinase inhibitors.
- To highlight how fluorescence can reveal drug-target interactions, binding sites, and dynamics.
- To underscore the potential of fluorescence in developing improved kinase-targeted therapies.
Main Methods:
- Review of spectroscopic approaches, focusing on fluorescence.
- Analysis of fluorescence's sensitivity to molecular environments and drug-target interactions.
- Exploration of fluorescence for studying structural properties, binding, kinetics, and dynamics of kinase inhibitors.
Main Results:
- Fluorescence spectroscopy provides detailed information on drug-target interactions.
- It can uncover hidden molecular conformations in both solution and bound states.
- Key binding properties like site location, hydrogen bonding, and hydrophobicity can be elucidated.
Conclusions:
- Fluorescence is a powerful tool for understanding kinase inhibitor behavior.
- Insights from intrinsic fluorescence can guide the design of future kinase inhibitors.
- This approach may lead to drugs with enhanced efficacy, reduced side effects, and less resistance.
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