Noninvasive evaluation of PD-L1 expression using Copper 64 labeled peptide WL12 by micro-PET imaging in Chinese hamster ovary cell tumor model.

Abstract

As an indicative biomarker for immunotherapy, PD-L1 plays an important role in the clinical decision-making of the immune checkpoint blockade therapy. PET imaging through radiotracer can real-timely, quantitatively, and non-invasively assess the expression of PD-L1 in tumors. Here, we reported a copper-64 radiolabeled NOTA-WL12, 64Cu-NOTA-WL12, and preliminarily evaluated its application in non-invasively detecting the PD-L1 expression.64Cu-NOTA-WL12 was produced with high radiochemical yield (>90%), radiochemical purity (>98%), and specific activity (20 MBq/nmol). 64Cu-NOTA-WL12 showed high in vitro stability and high binding affinity to the PD-L1 (KD ≈ 3.012 nM). The micro-positron emission tomography/computerized tomography (micro-PET/CT) imaging indicated that 64Cu-NOTA-WL12 was specifically accumulated in the tumor with PD-L1 expression. All results demonstrated that 64Cu-NOTA-WL12 holds great potential for noninvasive evaluation of PD-L1 expression levels.

• Authors: Jinquan Jiang, Dan Li, Teli Liu, Lei Xia, Xiaoyi Guo, Xiangxi Meng, Futao Liu, Feng Wang, Zhi Yang, Hua Zhu
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 40 Pg. 127901 (05 15 2021) ISSN: 1464-3405 [Electronic] England
• PMID: 33705912 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2021 Elsevier Ltd. All rights reserved.

Chemical References

• B7-H1 Antigen
• Copper Radioisotopes
• Copper-64
• Peptides
• Radiopharmaceuticals

Topics

• Animals
• B7-H1 Antigen (analysis, genetics)
• CHO Cells
• Copper Radioisotopes (economics)
• Cricetulus
• Gene Expression
• Humans
• Neoplasms, Experimental
• Peptides (chemistry)
• Positron Emission Tomography Computed Tomography
• Protein Binding
• Radiopharmaceuticals (chemistry)
• Staining and Labeling
• Structure-Activity Relationship