ArticleAnalytical biochemistry2007
Identification of inhibitors using a cell-based assay for monitoring Golgi-resident protease activity.
Article in Analytical biochemistry, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
19 citing papers in PubMed, 38 citations in OpenAlex.
- Towards a Survival-Based Cellular Assay for the Selection of Protease Inhibitors inBiotech (Basel (Switzerland)) · 2025Article
- Development and Prospects of Furin Inhibitors for Therapeutic Applications.International journal of molecular sciences · 2024Review
- Evaluation of Potential Furin Protease Inhibitory Properties of Pioglitazone, Rosiglitazone, and Pirfenidone: An In Silico Docking and Molecular Dynamics Simulation Approach.Current issues in molecular biology · 2024Article
- Discovery of diminazene as a dual inhibitor of SARS-CoV-2 human host proteases TMPRSS2 and furin using cell-based assays.Current research in chemical biology · 2022Article
- Furin Inhibitors Block SARS-CoV-2 Spike Protein Cleavage to Suppress Virus Production and Cytopathic Effects.Cell reports · 2020Article
- Identification of potent and compartment-selective small molecule furin inhibitors using cell-based assays.Biochemical pharmacology · 2015Article
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- Generation and characterization of non-competitive furin-inhibiting nanobodies.The Biochemical journal · 2012Article
- MScreen: an integrated compound management and high-throughput screening data storage and analysis system.Journal of biomolecular screening · 2012Article
- On the cutting edge of proprotein convertase pharmacology: from molecular concepts to clinical applications.Biomolecular concepts · 2011Article
- Molecular Validation of PACE4 as a Target in Prostate Cancer.Translational oncology · 2011Article
- Imaging proprotein convertase activities and their regulation in the implanting mouse blastocyst.The Journal of cell biology · 2010Article
- Applications of molecular imaging.Progress in molecular biology and translational science · 2010Review
- A novel enediynyl peptide inhibitor of furin that blocks processing of proPDGF-A, B and proVEGF-C.PloS one · 2009Article
- Inhibition of furin/proprotein convertase-catalyzed surface and intracellular processing by small molecules.The Journal of biological chemistry · 2009Article
- Synthetic small-molecule prohormone convertase 2 inhibitors.Molecular pharmacology · 2009Article
- Noninvasive imaging of apoptosis and its application in cancer therapeutics.Clinical cancer research : an official journal of the American Association for Cancer Research · 2008Article
- A small-molecule furin inhibitor inhibits cancer cell motility and invasiveness.Neoplasia (New York, N.Y.) · 2008Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Noninvasive real-time quantification of cellular protease activity allows monitoring of enzymatic activity and identification of activity modulators within the protease's natural milieu. We developed a protease activity assay based on differential localization of a recombinant reporter consisting of a Golgi retention signal and a protease cleavage sequence fused to alkaline phosphatase (AP). When expressed in mammalian cells, this protein localizes to Golgi bodies and, on protease-mediated cleavage, AP translocates to the extracellular medium where its activity is measured. We used this system to monitor the Golgi-associated protease furin, a pluripotent enzyme with a key role in tumorigenesis, viral propagation of avian influenza, ebola, and HIV as well as in activation of anthrax, pseudomonas, and diphtheria toxins. This technology was adapted for high-throughput screening of 39,000-compound small molecule libraries, leading to identification of furin inhibitors. Furthermore, this strategy was used to identify inhibitors of another Golgi protease, the beta-site amyloid precursor protein (APP)-cleaving enzyme (BACE). BACE cleavage of the APP leads to formation of the Abeta peptide, a key event that leads to Alzheimer's disease. In conclusion, we describe a customizable noninvasive technology for real-time assessment of Golgi protease activity used to identify inhibitors of furin and BACE.
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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.