ArticleCancers2023
Design and Biological Evaluation of Small-Molecule PET-Tracers for Imaging of Programmed Death Ligand 1.
Article in Cancers, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
15 citing papers in PubMed, 26 citations in OpenAlex.
- Dual-modal tumor-selective benzofuran tracer integrating real-time imaging and anticancer effects.Acta pharmaceutica Sinica. B · 2026Article
- Advances in GPCR-Targeted PET Radiotracer Patents (2020-2025).Pharmaceuticals (Basel, Switzerland) · 2026Review
- Synthesis and preclinical evaluation of small molecule-based radiotracers for PET imaging of PD-L1 expression and dynamics.European journal of nuclear medicine and molecular imaging · 2025Article
- Structure-activity relationship ofEJNMMI radiopharmacy and chemistry · 2025Article
- RadiolabeledFrontiers in nuclear medicine · 2025Article
- Imaging of tumor-associated macrophage dynamics during immunotherapy using a CD163-specific nanobody-based immunotracer.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- Bioorthogonal Diels-Alder Click Chemistry-Based Pretargeted PET Imaging Strategy for Monitoring Programmed Death-Ligand 1 Expression.ACS omega · 2024Article
- Development andJournal of medicinal chemistry · 2024Article
- Chelator impact: investigating the pharmacokinetic behavior of copper-64 labeled PD-L1 radioligands.EJNMMI radiopharmacy and chemistry · 2024Article
- Package delivered: folate receptor-mediated transporters in cancer therapy and diagnosis.Chemical science · 2024Review
- ImmunoPET provides a novel way to visualize the CD103EJNMMI research · 2024Review
- Design, Synthesis, and Biological Evaluation of Small-Molecule-Based Radioligands with Improved Pharmacokinetic Properties for Imaging of Programmed Death Ligand 1.Journal of medicinal chemistry · 2023Article
- Development and Preclinical Evaluation of [Pharmaceuticals (Basel, Switzerland) · 2023Article
- Exploring Hydrophilic PD-L1 Radiotracers Utilizing Phosphonic Acids: Insights into Unforeseen Pharmacokinetics.International journal of molecular sciences · 2023Article
- Chemokine receptor PET imaging: Bridging molecular insights with clinical applications.Nuclear medicine and biologyReview
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Noninvasive molecular imaging of the PD-1/PD-L1 immune checkpoint is of high clinical relevance for patient stratification and therapy monitoring in cancer patients. Here we report nine small-molecule PD-L1 radiotracers with solubilizing sulfonic acids and a linker-chelator system, designed by molecular docking experiments and synthesized according to a new, convergent synthetic strategy. Binding affinities were determined both in cellular saturation and real-time binding assay (LigandTracer), revealing dissociation constants in the single digit nanomolar range. Incubation in human serum and liver microsomes proved in vitro stability of these compounds. Small animal PET/CT imaging, in mice bearing PD-L1 overexpressing and PD-L1 negative tumors, showed moderate to low uptake. All compounds were cleared primarily through the hepatobiliary excretion route and showed a long circulation time. The latter was attributed to strong blood albumin binding effects, discovered during our binding experiments. Taken together, these compounds are a promising starting point for further development of a new class of PD-L1 targeting radiotracers.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.