ArticleBioconjugate chemistry2016
PET Imaging of Extracellular pH in Tumors with (64)Cu- and (18)F-Labeled pHLIP Peptides: A Structure-Activity Optimization Study.
Article in Bioconjugate chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers.
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Who cites it
41 citing papers in PubMed, 65 citations in OpenAlex.
- A multiparametric [European journal of nuclear medicine and molecular imaging · 2019Trial
- Lactate signaling and immune suppression in tumors: mechanisms and therapeutic implications.Cellular oncology (Dordrecht, Netherlands) · 2026Review
- A responsive Co(II)Chemical communications (Cambridge, England) · 2026Article
- Non-invasive visualization of pH changes within the tumor-micro-environment by positron emission tomography.EJNMMI research · 2026Article
- The Role of Tumor pH in Breast Cancer Imaging: Biology, Diagnostic Applications, and Emerging Techniques.Diagnostics (Basel, Switzerland) · 2025Review
- Small animal PET imaging with theEJNMMI radiopharmacy and chemistry · 2024Article
- Aiming the magic bullet: targeted delivery of imaging and therapeutic agents to solid tumors by pHLIP peptides.Frontiers in pharmacology · 2024Review
- Recent Advances in Imaging Agents Anchored with pH (Low) Insertion Peptides for Cancer Theranostics.Molecules (Basel, Switzerland) · 2023Review
- Monitor Tumor pHe and Response Longitudinally during Treatment Using CEST MRI-Detectable Alginate Microbeads.ACS applied materials & interfaces · 2022Article
- Increasing the Realism ofJournal of chemical theory and computation · 2022Article
- Article
- Radionuclide imaging and therapy directed towards the tumor microenvironment: a multi-cancer approach for personalized medicine.European journal of nuclear medicine and molecular imaging · 2022Review
- ES-MION-Based Dual-Modality PET/MRI Probes for Acidic Tumor Microenvironment Imaging.ACS omega · 2022Article
- In Vivo Distribution and Therapeutic Efficacy of Radioiodine-Labeled pH-Low Insertion Peptide Variant 3 in a Mouse Model of Breast Cancer.Molecular imaging · 2022Article
- Eradication of tumors and development of anti-cancer immunity using STINGa targeted by pHLIP.Frontiers in oncology · 2022Article
- PET Imaging of Acidic Tumor Environment WithFrontiers in oncology · 2022Article
- Synthesis and Evaluation of Technetium-99m-Labeled pH (Low) Insertion Peptide Variant 7 for Early Diagnosis of MDA-MB-231 Triple-Negative Breast Cancer by Targeting the Tumor Microenvironment.Frontiers in oncology · 2022Article
- Novel Tracers and Radionuclides in PET Imaging.Radiologic clinics of North America · 2021Review
- Review
- Dynamic Contrast Enhanced-MR CEST Urography: An Emerging Tool in the Diagnosis and Management of Upper Urinary Tract Obstruction.Tomography (Ann Arbor, Mich.) · 2021Review
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Authors and funding
13 authors at 3 institutions in 1 country.
Funding
Abstract
pH (low) insertion peptides (pHLIP peptides) target acidic extracellular environments in vivo due to pH-dependent cellular membrane insertion. Two variants (Var3 and Var7) and wild-type (WT) pHLIP peptides have shown promise for in vivo imaging of breast cancer. Two positron emitting radionuclides ((64)Cu and (18)F) were used to label the NOTA- and NO2A-derivatized Var3, Var7, and WT peptides for in vivo biodistribution studies in 4T1 orthotopic tumor-bearing BALB/c mice. All of the constructs were radiolabeled with (64)Cu or [(18)F]-AlF in good yield. The in vivo biodistribution of the 12 constructs in 4T1 orthotopic allografted female BALB/c mice indicated that NO2A-cysVar3, radiolabeled with either (18)F (4T1 uptake; 8.9 ± 1.7%ID/g at 4 h p.i.) or (64)Cu (4T1 uptake; 8.2 ± 0.9%ID/g at 4 h p.i. and 19.2 ± 1.8% ID/g at 24 h p.i.), shows the most promise for clinical translation. Additional studies to investigate other tumor models (melanoma, prostate, and brain tumor models) indicated the universality of tumor targeting of these tracers. From this study, future clinical translation will focus on (18)F- or (64)Cu-labeled NO2A-cysVar3.
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