2. Academic Validation
  3. Click Covalent-Targeted Radionuclide Therapy for Prostate Cancer

Click Covalent-Targeted Radionuclide Therapy for Prostate Cancer

  • J Med Chem. 2025 Aug 28;68(16):17794-17807. doi: 10.1021/acs.jmedchem.5c01515.
Weipeng Yong 1,  Shu Zhang 2,  Zhoudong Zhang 3,  Zhihao Li 1,  Yu Qin 1,  Xunhao Qi 1,  Dong Wang 1,  Yujuan Zhang 4,  Jianguo Li 2,  Zhiyong Liu 1,  Ran Zhu 1,  Huanqiu Li 3,  Guanglin Wang 1
Affiliations

Affiliations

  • 1 State Key Laboratory of Radiation Medicine and Protection, School of Radiation Medicine and Protection, Collaborative Innovation Center of Radiation Medicine of Jiangsu Higher Education Institutions, Soochow University, Suzhou 215123, China.
  • 2 Division of Radiation Medicine and Environmental Medicine, CAEA Center of Excellence on Nuclear Technology Applications for Nonclinical Evaluation for Radiopharmaceutical, CNNC Key Laboratory on Radio-Toxicology and Radiopharmaceutical Preclinical Evaluation, Shanxi Key Laboratory of Drug Toxicology and Preclinical Studies for Radiopharmaceutical, China Institute for Radiation Protection, Taiyuan 030006, China.
  • 3 Jiang Su Key Laboratory of Antibody-Targeted Drug Research, College of Pharmaceutical Sciences, Soochow University, Suzhou 215123, China.
  • 4 Experimental Center of Soochow University, Department of Medicine, Soochow University, Suzhou 215123, PR China.
PMID: 40787824 DOI: 10.1021/acs.jmedchem.5c01515
Abstract

Targeted radionuclide therapy represents a promising therapeutic method for treating Cancer. However, currently approved radioligands still require improvement in terms of tumor uptake and retention. This study employed molecular simulation to design a novel radioligand, designated PSMA-MAL-5, which covalently binds to the prostate-specific membrane antigen (PSMA). This ligand can be efficiently radiolabeled with the beta emitter (177Lu) and the alpha emitter (225Ac) and exhibits a high level of radiostability. Autoradiography confirmed that 177Lu-PSMA-MAL-5 binds covalently to PSMA. In vivo experiments demonstrated that the radioligand can effectively target PSMA-positive tumors, with an area under the curve of tumor uptake higher than that observed for 177Lu-PSMA-617 (2517 ± 499 h %ID/cm3 vs 575 ± 75 h %ID/cm3). Tumor inhibition studies indicated that the radioligand exhibited a notable tumor inhibitory effect on tumor growth, showing promise as a tool for targeted radionuclide therapy of PSMA-positive prostate Cancer.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-175744
    PSMA配体
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