Preparation and Characterization of a Caspase-3 Targeted PET Molecular Probe
ZHANG Lixia1,2, XU Liang1,2, LI Huirong1,2, LIANG Beibei1,2, LIN Jianguo1,2, QIU Ling1,2*
1. School of Basic Medical Sciences, Wenzhou Medical University, Wenzhou 325000, China; 2. NHC Key Laboratory of Nuclear Medicine, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China
Abstract：Inducing tumor cell apoptosis is one of the action mechanisms for several antitumor therapies. Therefore, detection of tumor cell apoptosis has become an important index to evaluate the therapeutic effect of tumor. Cell apoptosis-specific molecular probe was designed with caspase-3 as the target, and therapeutic efficacy could be timely evaluated by monitoring the expression level of caspase-3. In this study, a positron emission tomography (PET) probe [18F]8 targeting caspase-3 was reported. The polypeptide and precursor 8 were synthesized by simple solid-phase synthesis method and click chemistry method, respectively. The precursor 8 was labeled with 18F using 18F-19F isotope exchange method to obtain the probe [18F]8 with radiochemical yield of 16% and radiochemical purity of 95%. The probe displayed good stability in PBS and mouse serum, and the lipo-hydro partition coefficient (Log P) of the probe was determined to be -1.69 ± 0.01, suggesting that the probe was hydrophilic. The convenient synthesis method and good physicochemical properties provided a good basis for the application of the probe in PET imaging of tumor apoptosis.
[J]. 合成化学, 2023, 31(3): 177-185.
ZHANG Lixia, XU Liang, LI Huirong, LIANG Beibei, LIN Jianguo, QIU Ling. Preparation and Characterization of a Caspase-3 Targeted PET Molecular Probe. Chinese Journal of Synthetic Chemistry, 2023, 31(3): 177-185.
