Emissive Alkylated Guanine Analogs as Probes for Monitoring O ⁶-Alkylguanine-DNA-transferase Activity.

ABSTRACT: Human O ⁶-alkylguanine-DNA-transferase (hAGT) is a repair protein that provides protection from mutagenic events caused by O ⁶-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 O ⁶-methyl- and O ⁶-benzylguanine analogs based on our previously described ^th G _N and ^tz G _N , thieno- and isothiazolo-guanine surrogates, respectively, as potential reporters. We establish that

SUBMITTER: Steinbuch KB 

PROVIDER: S-EPMC11360037 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature