2. Academic Validation
  3. In vivo visualization of fluorescence reflecting CDK4 activity in a breast cancer mouse model

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

  • MedComm (2020). 2022 Jun 10;3(3):e136. doi: 10.1002/mco2.136.
Yi-Yang Gao 1 2 3 4,  Rui-Qin Yang 1 2 3 4,  Kang-Liang Lou 1 2 3 4,  Yong-Ying Dang 1 2 3 4,  Yuan-Yuan Dong 1 2 3 4,  Yue-Yang He 1 2 3 4,  Wen-He Huang 1 2 3 5,  Min Chen 3 4 6,  Guo-Jun Zhang 1 2 3 5 6
Affiliations

Affiliations

  • 1 Department of Breast and Thyroid Surgery Xiang'an Hospital of Xiamen University, School of Medicine, Xiamen University Xiamen China.
  • 2 Fujian Key Laboratory of Precision Diagnosis and Treatment in Breast Cancer Xiang'an Hospital of Xiamen University, Xiamen University Xiamen China.
  • 3 Xiamen Key Laboratory of Endocrine-Related Cancer Precision Medicine Xiang'an Hospital of Xiamen University, Xiamen University Xiamen China.
  • 4 Central Laboratory Xiang'an Hospital of Xiamen University, School of Medicine, Xiamen University Xiamen China.
  • 5 Xiamen Research Center of Clinical Medicine in Breast and Thyroid Cancers Xiang'an Hospital of Xiamen University, Xiamen University Xiamen China.
  • 6 Cancer Research Center of Xiamen University School of Medicine, Xiamen University Xiamen China.
PMID: 35711853 DOI: 10.1002/mco2.136
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 palbociclib treatment was significantly lower than that before treatment, while no significant change in tumor diameter was observed under magnetic resonance imaging. Overall, we developed an innovative fluorescent probe that can monitor CDK4 activity and the early therapeutic response to CDK4 inhibitors in living cells and in vivo. It may provide a new strategy for evaluating antitumor therapeutic efficacy in a clinical context and for drug development.

Keywords

CDK4 inhibitors; breast cancer; fluorescence imaging; kinase activity; therapeutic evaluation.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-50767
    99.94%, CDK4/6 Inhibitor
    CDK