ArticleChemical science2018
Selective imaging of cathepsin L in breast cancer by fluorescent activity-based probes.
Article in Chemical science, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
What it found
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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.
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.
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Who cites it
38 citing papers in PubMed, 85 citations in OpenAlex.
- Development and preclinical evaluation of selective vinyl sulfone-based probes for PET imaging of tumor-associated cathepsins.EJNMMI radiopharmacy and chemistry · 2026Article
- Engineering Cathepsin S Selective Chemical Probes and Antibody-Drug Conjugates through Substrate Profiling with Unnatural Amino Acids.Journal of medicinal chemistry · 2026Article
- Peptidomimetic α,β-Unsaturated Ethyl Esters Are Irreversible Inactivators of Human Cathepsin L and Are Potent Inhibitors of SARS-CoV-2 in Cellular Models of COVID-19.Journal of medicinal chemistry · 2026Article
- Chemical probes for enzyme imaging: challenges in design, synthesis and biomedical applications.Chemical science · 2025Review
- Article
- Avellanin A Has an Antiproliferative Effect on TP-Induced RWPE-1 Cells via the PI3K-Akt Signalling Pathway.Marine drugs · 2024Article
- Thermoprotection by a cell membrane-localized metacaspase in a green alga.The Plant cell · 2024Article
- Integrative transcriptomic and network pharmacology analysis reveals the neuroprotective role of BYHWD through enhancing autophagy by inhibiting Ctsb in intracerebral hemorrhage mice.Chinese medicine · 2023Article
- Chemical Tools to Image the Activity of PAR-Cleaving Proteases.ACS bio & med chem Au · 2023Review
- Selection of an Amino Acid Site with One of the Fastest Cleavage Kinetics by the Endosomal Protease Cathepsin B for Potential Use in Drug Delivery Systems.Doklady. Biochemistry and biophysics · 2023Article
- Fluorescent Activity-Based Probe To Image and Inhibit Factor XIa Activity in Human Plasma.Journal of medicinal chemistry · 2023Article
- Cysteine Cathepsins in Breast Cancer: Promising Targets for Fluorescence-Guided Surgery.Molecular imaging and biology · 2023Review
- Design and Synthesis of Ubiquitin-Based Chemical Tools with Unnatural Amino Acids for Selective Detection of Deubiquitinases.Methods in molecular biology (Clifton, N.J.) · 2023Article
- A KLK6 Activity-Based Probe Reveals a Role for KLK6 Activity in Pancreatic Cancer Cell Invasion.Journal of the American Chemical Society · 2022Article
- Chemically diverse activity-based probes with unexpected inhibitory mechanisms targeting trypsin-like serine proteases.Frontiers in chemistry · 2022Article
- Methionine deprivation inhibits glioma growth through downregulation of CTSL.American journal of cancer research · 2022Article
- Inhibition of Serine Proteases as a Novel Therapeutic Strategy for Abdominal Pain in IBS.Frontiers in physiology · 2022Review
- Lessons in Organic Fluorescent Probe Discovery.Chembiochem : a European journal of chemical biology · 2021Review
- Near-Infrared Fluorescent Probes for the Detection of Cancer-Associated Proteases.ACS chemical biology · 2021Review
- Molecular probes for selective detection of cysteine cathepsins.Organic & biomolecular chemistry · 2021Review
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 4 countries.
Funding
Abstract
Cysteine cathepsins normally function in the lysosomal degradation system where they are critical for the maintenance of cellular homeostasis and the MHC II immune response, and have been found to have major roles in several diseases and in tumor progression. Selective visualization of individual protease activity within a complex proteome is of major importance to establish their roles in both normal and tumor cells, thereby facilitating our understanding of the regulation of proteolytic networks. A generally accepted means to monitor protease activity is the use of small molecule substrates and activity-based probes. However, there are eleven human cysteine cathepsins, with a few of them displaying overlapping substrate specificity, making the development of small molecules that selectively target a single cathepsin very challenging. Here, we utilized HyCoSuL, a positional scanning substrate approach, to develop a highly-selective fluorogenic substrate and activity-based probe for monitoring cathepsin L activity in the breast cancer cell line MDA-MB-231. Use of this probe enabled us to distinguish the activity of cathepsin L from that of other cathepsins, particularly cathepsin B, which is abundant and ubiquitously expressed in normal and transformed cell types. We found that cathepsin L localization in MDA-MB-231 cells greatly overlaps with that of cathepsin B, however, several cathepsin L-rich lysosomes lacked cathepsin B activity. Overall, these studies demonstrate that HyCoSuL-derived small molecule probes are valuable tools to image cathepsin L activity in living cells. This approach thus enables evaluation of cathepsin L function in tumorigenesis and is applicable to other cysteine cathepsins.
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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.