ArticleProceedings of the National Academy of Sciences of the United States of America2014
Understanding the pharmacological properties of a metabolic PET tracer in prostate cancer.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed, 47 citations in OpenAlex.
- Aiming the magic bullet: targeted delivery of imaging and therapeutic agents to solid tumors by pHLIP peptides.Frontiers in pharmacology · 2024Review
- Recent Advances of Studies on Cell-Penetrating Peptides Based on Molecular Dynamics Simulations.Cells · 2022Review
- Recent advances in developing active targeting and multi-functional drug delivery systems via bioorthogonal chemistry.Signal transduction and targeted therapy · 2022Review
- Article
- Microenvironment-triggered multimodal precision diagnostics.Nature materials · 2021Article
- Pharmacokinetic modeling reveals parameters that govern tumor targeting and delivery by a pH-Low Insertion Peptide (pHLIP).Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- An Experimental Study on [Molecular imaging · 2021Article
- Microenvironment Stimulated Bioresponsive Small Molecule Carriers for Radiopharmaceuticals.ACS omega · 2020Review
- Using Simulation to Understand the Role of Titration on the Stability of a Peptide-Lipid Bilayer Complex.Langmuir : the ACS journal of surfaces and colloids · 2020Article
- Targeting tumor-associated acidity in cancer immunotherapy.Cancer immunology, immunotherapy : CII · 2018Review
- Carbonic anhydrase IX is a pH-stat that sets an acidic tumour extracellular pH in vivo.British journal of cancer · 2018Article
- Bilayer Thickness and Curvature Influence Binding and Insertion of a pHLIP Peptide.Biophysical journal · 2018Article
- CAIX aptamer-functionalized targeted nanobubbles for ultrasound molecular imaging of various tumors.International journal of nanomedicine · 2018Article
- Applications of pHLIP Technology for Cancer Imaging and Therapy.Trends in biotechnology · 2017Review
- Investigation of endosome and lysosome biology by ultra pH-sensitive nanoprobes.Advanced drug delivery reviews · 2017Review
- Characterization of the Tumor Microenvironment and Tumor-Stroma Interaction by Non-invasive Preclinical Imaging.Frontiers in oncology · 2017Review
- Insertion into lipid bilayer of truncated pHLIPBiochemistry and biophysics reports · 2016Article
- pHLIP Peptide Interaction with a Membrane Monitored by SAXS.The journal of physical chemistry. B · 2016Article
- Comparative Study of Tumor Targeting and Biodistribution of pH (Low) Insertion Peptides (pHLIP(®) Peptides) Conjugated with Different Fluorescent Dyes.Molecular imaging and biology · 2016Article
- PET Imaging of Extracellular pH in Tumors with (64)Cu- and (18)F-Labeled pHLIP Peptides: A Structure-Activity Optimization Study.Bioconjugate chemistry · 2016Article
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14 authors at 4 institutions in 3 countries.
Funding
Abstract
Generally, solid tumors (>400 mm(3)) are inherently acidic, with more aggressive growth producing greater acidity. If the acidity could be targeted as a biomarker, it would provide a means to gauge the pace of tumor growth and degree of invasiveness, as well as providing a basis for predicting responses to pH-dependent chemotherapies. We have developed a (64)Cu pH (low) insertion peptide (pHLIP) for targeting, imaging, and quantifying acidic tumors by PET, and our findings reveal utility in assessing prostate tumors. The new pHLIP version limits indiscriminate healthy tissue binding, and we demonstrate its targeting of extracellular acidification in three different prostate cancer models, each with different vascularization and acid-extruding protein carbonic anhydrase IX (CAIX) expression. We then describe the tumor distribution of this radiotracer ex vivo, in association with blood perfusion and known biomarkers of acidity, such as hypoxia, lactate dehydrogenase A, and CAIX. We find that the probe reveals metabolic variations between and within tumors, and discriminates between necrotic and living tumor areas.
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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.