In vivo visualization of fluorescence reflecting CDK4 activity in a breast cancer mouse model.

ABSTRACT: The CDK4/6-Rb axis is a crucial target of cancer therapy and several selective inhibitors of it have been approved for clinical application. However, current therapeutic efficacy evaluation mostly relies on anatomical imaging, which cannot directly reflect changes in drug targets, leading to a delay in the selection of optimal treatment. In this study, we constructed a novel fluorescent probe, CPP30-Lipo/CDKACT4, for real-time monitoring of CDK4 activity and the therapeutic efficacy of its inhibitor in HR⁺/HER2^- breast cancer. CPP30-Lipo/CDKACT4 exhibited good optical stability and targetability. The signal of the probe in living cells decreased after CDK4 knockdown or palbociclib treatment. Moreover, the fluorescence intensity of the tumors after 7 days of palbocicli

SUBMITTER: Gao YY 

PROVIDER: S-EPMC9187519 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature