ArticleBioconjugate chemistry2016
Caged [(18)F]FDG Glycosylamines for Imaging Acidic Tumor Microenvironments Using Positron Emission Tomography.
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 25 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
25 citing papers in PubMed, 39 citations in OpenAlex.
- Non-invasive visualization of pH changes within the tumor-micro-environment by positron emission tomography.EJNMMI research · 2026Article
- The Impact of Tumor Microenvironmental Acidity on Bicalutamide Sensitivity in Prostate Cancer Cells.Prostate cancer · 2026Article
- Glucose stimulated CEST MRI pHe mapping for improved differentiation of tumors with altered hypoxia inducible factor 1alpha expression.Scientific reports · 2025Article
- CD46-Targeted Theranostics for PET and 225Ac-Radiopharmaceutical Therapy of Multiple Myeloma.Clinical cancer research : an official journal of the American Association for Cancer Research · 2024Article
- Chemoenzymatic Syntheses of Fluorine-18-Labeled Disaccharides from [Journal of the American Chemical Society · 2023Article
- Fluorinated carbohydrates forChemical Society reviews · 2023Review
- 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
- Sweetening Pharmaceutical Radiochemistry byPharmaceuticals (Basel, Switzerland) · 2021Review
- Current Trends in Non-Invasive Imaging of Interactions in the Liver Tumor Microenvironment Mediated by Tumor Metabolism.Cancers · 2021Review
- Tumor Microenvironment Biosensors for Hyperpolarized Carbon-13 Magnetic Resonance Spectroscopy.Molecular imaging and biology · 2021Review
- Imaging methods to evaluate tumor microenvironment factors affecting nanoparticle drug delivery and antitumor response.Cancer drug resistance (Alhambra, Calif.) · 2021Article
- Microenvironment Stimulated Bioresponsive Small Molecule Carriers for Radiopharmaceuticals.ACS omega · 2020Review
- How and Why Are Cancers Acidic? Carbonic Anhydrase IX and the Homeostatic Control of Tumour Extracellular pH.Cancers · 2020Review
- Increased Tumoral Microenvironmental pH Improves Cytotoxic Effect of Pharmacologic Ascorbic Acid in Castration-Resistant Prostate Cancer Cells.Frontiers in pharmacology · 2020Article
- Cellular and Extracellular Components in Tumor Microenvironment and Their Application in Early Diagnosis of Cancers.Analytical cellular pathology (Amsterdam) · 2020Review
- Activity-Based Sensing Methods for Monitoring the Reactive Carbon Species Carbon Monoxide and Formaldehyde in Living Systems.Accounts of chemical research · 2019Review
- Spatiotemporal pH Heterogeneity as a Promoter of Cancer Progression and Therapeutic Resistance.Cancers · 2019Review
- Transistor-like Ultra-pH-Sensitive Polymeric Nanoparticles.Accounts of chemical research · 2019Review
- Imaging tumor acidosis: a survey of the available techniques for mapping in vivo tumor pH.Cancer metastasis reviews · 2019Review
- Targeting tumor-associated acidity in cancer immunotherapy.Cancer immunology, immunotherapy : CII · 2018Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors at 3 institutions in 1 country.
Funding
Abstract
Solid tumors are hypoxic with altered metabolism, resulting in secretion of acids into the extracellular matrix and lower relative pH, a feature associated with local invasion and metastasis. Therapeutic and diagnostic agents responsive to this microenvironment may improve tumor-specific delivery. Therefore, we pursued a general strategy whereby caged small-molecule drugs or imaging agents liberate their parent compounds in regions of low interstitial pH. In this manuscript, we present a new acid-labile prodrug method based on the glycosylamine linkage, and its application to a class of positron emission tomography (PET) imaging tracers, termed [(18)F]FDG amines. [(18)F]FDG amines operate via a proposed two-step mechanism, in which an acid-labile precursor decomposes to form the common radiotracer 2-deoxy-2-[(18)F]fluoro-d-glucose, which is subsequently accumulated by glucose avid cells. The rate of decomposition of [(18)F]FDG amines is tunable in a systematic fashion, tracking the pKa of the parent amine. In vivo, a 4-phenylbenzylamine [(18)F]FDG amine congener showed greater relative accumulation in tumors over benign tissue, which could be attenuated upon tumor alkalinization using previously validated models, including sodium bicarbonate treatment, or overexpression of carbonic anhydrase. This new class of PET tracer represents a viable approach for imaging acidic interstitial pH with potential for clinical translation.
Indexed as
Identifiers
What OpenQuestion holds
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.