Synthesis and Imaging of Novel CDK19‐Targeted Tracers Incorporating an Albumin‐Binding Moiety
Cyclin-dependent kinase 19 (CDK19) is a potential target for the diagnosis and treatment of prostate cancer. We have previously studied a series of CDK19-targeted PET tracers, but in-depth drug optimization is needed to improve the physiochemical properties of such large and polar tracers. The albumin strategy has received widespread attention in recent years, and we synthesized <sup>68</sup>Ga-IRM-14a and <sup>68</sup>Ga-IRM-14b based on the strategy. After in vivo imaging studies in mice, we found that introducing albumin moiety will significantly change the physicochemical properties of existing large polarity tracers, thereby increasing tissue uptake and retention, which is beneficial for future treatment. In short, the albumin strategy will be an important strategy in the field of radiopharmaceutical optimization.
Authors
- Wenbin Hou (ORCID: https://orcid.org/0000-0001-6527-975X)
- Yanli Li (ORCID: https://orcid.org/0000-0002-2936-0339)
- Panfeng Li (ORCID: https://orcid.org/0000-0001-8586-0648)
- Ziyang Wang (ORCID: https://orcid.org/0000-0002-3174-1894)
- Dong Dai (ORCID: https://orcid.org/0000-0003-1278-5581)
- Xiaoman Liu
- Yu Jiang (ORCID: https://orcid.org/0009-0002-5487-1701)
- Yu Zhao (ORCID: https://orcid.org/0000-0002-1242-2257)
- Yiliang Li (ORCID: https://orcid.org/0000-0002-3592-6167)
- Zhao Yang
- Jun Nie
Institutions
- Tianjin University of Traditional Chinese Medicine (CN)
- Chinese Academy of Medical Sciences & Peking Union Medical College (CN)
- Tianjin Medical University Cancer Institute and Hospital (CN)
Publication Details
- Journal
- Journal of Labelled Compounds and Radiopharmaceuticals
- Published
- 2025-03-01
- DOI
- https://doi.org/10.1002/jlcr.4130
- Primary Topic
- Prostate Cancer Treatment and Research
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Natural Science Foundation of China