ArticleBioorganic & medicinal chemistry letters2019
Structure-based design, synthesis and biological evaluation of a novel series of isoquinolone and pyrazolo[4,3-c]pyridine inhibitors of fascin 1 as potential anti-metastatic agents.
Article in Bioorganic & medicinal chemistry letters, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 22 citations in OpenAlex.
- High Expression of Actin Binding Proteins Predicts Hematogenous Metastases in Non-Small Cell Lung Cancer.Asian Pacific journal of cancer prevention : APJCP · 2025Article
- Nootropic benzothiazoles promote dendritic spine formation by targeting fascin-1.The Journal of biological chemistry · 2025Article
- Structural insights into full-length human fascin1: a target for cancer treatment.Acta crystallographica. Section F, Structural biology communications · 2025Article
- CrypTothML: An Integrated Mixed-Solvent Molecular Dynamics Simulation and Machine Learning Approach for Cryptic Site Prediction.International journal of molecular sciences · 2025Article
- A nanobody inhibitor of Fascin-1 actin-bundling activity and filopodia formation.Open biology · 2024Article
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- Dess-Martin Periodinane-Mediated Oxidative Coupling Reaction of Isoquinoline with Benzyl Bromide.Molecules (Basel, Switzerland) · 2023Article
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- Fascin-1: Updated biological functions and therapeutic implications in cancer biology.BBA advances · 2022Review
- Review
- Fascin promotes lung cancer growth and metastasis by enhancing glycolysis and PFKFB3 expression.Cancer letters · 2021Article
- Isoquinolone-4-Carboxylic Acids by Ammonia-Ugi-4CR and Copper-Catalyzed Domino Reaction.The Journal of organic chemistry · 2021Article
- Fascin1 empowers YAP mechanotransduction and promotes cholangiocarcinoma development.Communications biology · 2021Article
- Fascin actin-bundling protein 1 in human cancer: promising biomarker or therapeutic target?Molecular therapy oncolytics · 2021Review
- How does fascin promote cancer metastasis?The FEBS journal · 2021Review
- Potential Inhibitors of Fascin From A Database of Marine Natural Products: A Virtual Screening and Molecular Dynamics Study.Frontiers in chemistry · 2021Article
- Review
- Palladium-catalyzed regio- and stereoselective synthesis of aryl and 3-indolyl-substituted 4-methylene-3,4-dihydroisoquinolin-1(Beilstein journal of organic chemistry · 2020Article
Corrections and comments
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Authors and funding
20 authors at 1 institution in 1 country.
Funding
Abstract
Fascin is an actin binding and bundling protein that is not expressed in normal epithelial tissues but overexpressed in a variety of invasive epithelial tumors. It has a critical role in cancer cell metastasis by promoting cell migration and invasion. Here we report the crystal structures of fascin in complex with a series of novel and potent inhibitors. Structure-based elaboration of these compounds enabled the development of a series with nanomolar affinities for fascin, good physicochemical properties and the ability to inhibit fascin-mediated bundling of filamentous actin. These compounds provide promising starting points for fascin-targeted anti-metastatic therapies.
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Registered trials
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