ArticleACS chemical biology2015
Design of Protease Activated Optical Contrast Agents That Exploit a Latent Lysosomotropic Effect for Use in Fluorescence-Guided Surgery.
Article in ACS chemical biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 58 papers, 1 of them a synthesis that pooled it.
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
58 citing papers in PubMed, 1 synthesis or guideline pooled it, 119 citations in OpenAlex.
- Pooled it
- Chemical basis of fluorogenic substrate probe design: revisiting the past to discover the new in biochemistry.RSC chemical biology · 2026Review
- Chemiluminescent probes for imaging cysteine cathepsin activity.Bioorganic & medicinal chemistry letters · 2026Article
- Chemical probes for enzyme imaging: challenges in design, synthesis and biomedical applications.Chemical science · 2025Review
- Identifying protease-activated targets and exploring therapeutic applications.Expert opinion on therapeutic targets · 2025Review
- Biodistribution-Driven Discovery Identifies a Glycosidase-Cleavable Linker to Reprogram Radiotheranostics.bioRxiv : the preprint server for biology · 2025Article
- Protease engineering: Approaches, tools, and emerging trends.Biotechnology advances · 2025Review
- Polymer-Tethered Quenched Fluorescent Probes for Enhanced Imaging of Tumor-Associated Proteases.ACS sensors · 2024Article
- Recent advances in ratiometric fluorescence imaging of enzyme activity in vivo.Current opinion in chemical biology · 2024Review
- Polymer-tethered quenched fluorescent probes for enhanced imaging of tumor associated proteases.bioRxiv : the preprint server for biology · 2024Article
- Ruthenium-Cathepsin Inhibitor Conjugates for Green Light-Activated Photodynamic Therapy and Photochemotherapy.Inorganic chemistry · 2024Article
- A radioactive and fluorescent dual modality cysteine cathepsin-B activity-based probe for the detection and treatment evaluation in rheumatoid arthritis.American journal of nuclear medicine and molecular imaging · 2024Article
- Targeted, Molecular EuropiumJournal of the American Chemical Society · 2023Article
- Protease Activated Probes for Real-Time Ratiometric Imaging of Solid Tumors.ACS central science · 2023Article
- Cysteine Cathepsins in Breast Cancer: Promising Targets for Fluorescence-Guided Surgery.Molecular imaging and biology · 2023Review
- A Cathepsin-Targeted Quenched Activity-Based Probe Facilitates Enhanced Detection of Human Tumors during Resection.Clinical cancer research : an official journal of the American Association for Cancer Research · 2022Article
- A versatile fluorescence-quenched substrate for quantitative measurement of glucocerebrosidase activity within live cells.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Article
- Near-Infrared Fluorescence Tumor-Targeted Imaging in Lung Cancer: A Systematic Review.Life (Basel, Switzerland) · 2022Review
- Progress on Multifunction Enzyme-Activated Organic Fluorescent Probes for Bioimaging.Frontiers in chemistry · 2022Review
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
There is a need for new molecular-guided contrast agents to enhance surgical procedures such as tumor resection that require a high degree of precision. Cysteine cathepsins are highly up-regulated in a wide variety of cancers, both in tumor cells and in the tumor-supporting cells of the surrounding stroma. Therefore, tools that can be used to dynamically monitor their activity in vivo could be used as imaging contrast agents for intraoperative fluorescence image guided surgery (FGS). Although multiple classes of cathepsin-targeted substrate probes have been reported, most suffer from overall fast clearance from sites of protease activation, leading to reduced signal intensity and duration in vivo. Here we describe the design and synthesis of a series of near-infrared fluorogenic probes that exploit a latent cationic lysosomotropic effect (LLE) to promote cellular retention upon protease activation. These probes show tumor-specific retention, fast activation kinetics, and rapid systemic distribution. We demonstrate that they are suitable for detection of diverse cancer types including breast, colon and lung tumors. Most importantly, the agents are compatible with the existing, FDA approved, da Vinci surgical system for fluorescence guided tumor resection. Therefore, our data suggest that the probes reported here can be used with existing clinical instrumentation to detect tumors and potentially other types of inflammatory lesions to guide surgical decision making in real time.
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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.