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Fluorescent kinase inhibitors as probes in cancer
Syed Muhammad Usama1, Bosheng Zhao, Kevin Burgess
1Department of Chemistry, Texas A&M University, Box 30012, College Station, TX 77842, USA. burgess@tamu.edu.
Abstract:
Fluorescent dyes attached to kinase inhibitors (KIs) can be used to probe kinases in vitro, in cells, and in vivo. Ideal characteristics of the dyes vary with their intended applications. Fluorophores used in vitro may inform on kinase active site environments, hence the dyes used should be small and have minimal impact on modes of binding. These probes may have short wavelength emissions since blue fluorophores are perfectly adequate in this context. Thus, for instance, KI fragments that mimic nucleobases may be modified to be fluorescent with minimal perturbation to the kinase inhibitor structure. However, progressively larger dyes, that emit at longer wavelengths, are required for cellular and in vivo work. In cells, it is necessary to have emissions above autofluorescence of biomolecules, and near infrared dyes are needed to enable excitation and observation through tissue in vivo. This review is organized to describe probes intended for applications in vitro, in cells, then in vivo. The readers will observe that the probes featured tend to become larger and responsive to the near infared end of the spectrum as the review progresses. Readers may also be surprised to realize that relatively few dyes have been used for fluorophore-kinase inhibitor conjugates, and the area is open for innovations in the types of fluorophores used.
Insights
Fluorescent dyes attached to kinase inhibitors (KIs) are versatile tools for studying kinases. Dye selection depends on the application, with larger, longer-wavelength dyes needed for cellular and in vivo imaging.
Area of Science:
- Biochemistry
- Chemical Biology
- Molecular Imaging
Background:
- Fluorescent dyes conjugated to kinase inhibitors (KIs) offer powerful methods for probing kinase activity.
- The ideal characteristics of these fluorescent probes, including dye size and emission wavelength, are application-dependent.
Purpose of the Study:
- To review the development and application of fluorescent dye-kinase inhibitor conjugates.
- To highlight how dye properties must be tailored for different biological contexts: in vitro, cellular, and in vivo studies.
Main Methods:
- Review of literature focusing on fluorophore-kinase inhibitor conjugates.
- Categorization of probes based on their intended application (in vitro, cellular, in vivo).
- Analysis of dye characteristics such as size, emission wavelength, and impact on kinase binding.
Main Results:
- Probes for in vitro studies are typically small, with short-wavelength emissions, minimizing interference with kinase binding.
- Cellular and in vivo applications necessitate larger dyes with longer emission wavelengths (including near-infrared) to overcome autofluorescence and enable tissue penetration.
- A limited range of fluorophores has been employed in this field, indicating significant room for innovation.
Conclusions:
- The choice of fluorescent dye for kinase inhibitor conjugates is critical and must align with the specific biological question and imaging environment.
- There is a clear trend towards larger, longer-wavelength dyes for more complex biological imaging.
- The field of fluorophore-kinase inhibitor conjugates is ripe for the exploration of novel dye chemistries and designs.
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