Reagents and methods for assessing levels of O⁶-alkylguanine-DNA alkyltransferase in vivo

摘要

Radiolabeled O<6>-derivatized guanine molecules can be used to form radiolabeled AGT molecules which can be detected in vivo. In vivo assessment of AGT levels is useful for optimizing the efficacy of chemotherapy. In addition, assessing AGT levels in tumors in vivo permits selection of patients most likely to benefit from such chemotherapy and enables clinicians to monitor the effect of known and potential chemotherapeutic agents. In particular, methods have been developed for the efficient syntheses of [<18>F]FBG and [<131>I]IBG, both of which bind specifically to purified AGT. These two radiolabeled O<6> benzylguanine analogues can be used to assess levels of AGT in vivo.