AI Article Synopsis
- hAGT is a key repair protein that protects against DNA damage from alkylguanine lesions and is linked to tumor status and chemotherapy effectiveness.
- Researchers are investigating new types of guanine analogs as tools to track hAGT activity for better disease diagnosis and treatment.
- Two specific analogs show promise for optical monitoring of hAGT activity and can be utilized in cell imaging techniques like fluorescence microscopy.
Article Abstract
Human -alkylguanine-DNA-transferase (hAGT) is a repair protein that provides protection from mutagenic events caused by -alkylguanine lesions. As this stoichiometric activity is tissue-specific, indicative of tumor status, and correlated to chemotherapeutic success, tracking the activity of hAGT could prove to be informative for disease diagnosis and therapy. Herein, we explore two families of emissive -methyl- and -benzylguanine analogs based on our previously described and , thieno- and isothiazolo-guanine surrogates, respectively, as potential reporters. We establish that and provide a spectral window to optically monitor hAGT activity, can be used as substrates for the widely used SNAP-Tag delivery system, and are sufficiently bright to be visualized in mammalian cells using fluorescence microscopy.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11360037 | PMC |
| http://dx.doi.org/10.1021/acsomega.4c05700 | DOI Listing |
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