ArticleChemistry & biology2010
A structure-guided approach to creating covalent FGFR inhibitors.
Article in Chemistry & biology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 54 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
54 citing papers in PubMed, 138 citations in OpenAlex.
- Computational Design of Lysine Targeting Covalent Binders Using Rosetta.Journal of chemical information and modeling · 2025Article
- Review
- Advances in reversible covalent kinase inhibitors.Medicinal research reviews · 2025Review
- Targeting the cancer cells and cancer-associated fibroblasts with next-generation FGFR inhibitors in prostate cancer co-culture models.Cancer medicine · 2024Article
- Targeting FGFR for cancer therapy.Journal of hematology & oncology · 2024Review
- Discovery of Futibatinib: The First Covalent FGFR Kinase Inhibitor in Clinical Use.ACS medicinal chemistry letters · 2023Article
- Developing a Kinase Chemogenomic Set: Facilitating Investigation into Kinase Biology by Linking Phenotypes to Targets.Methods in molecular biology (Clifton, N.J.) · 2023Article
- Alveolar cell fate selection and lifelong maintenance of AT2 cells by FGF signaling.Nature communications · 2022Article
- Identification of Slow-Binding Inhibitors of the BoNT/A Protease.ACS medicinal chemistry letters · 2022Article
- Structural insights into the potency and selectivity of covalent pan-FGFR inhibitors.Communications chemistry · 2022Article
- Nek2 Kinase Signaling in Malaria, Bone, Immune and Kidney Disorders to Metastatic Cancers and Drug Resistance: Progress on Nek2 Inhibitor Development.Molecules (Basel, Switzerland) · 2022Review
- Signaling Pathway and Small-Molecule Drug Discovery of FGFR: A Comprehensive Review.Frontiers in chemistry · 2022Review
- DW14383 is an irreversible pan-FGFR inhibitor that suppresses FGFR-dependent tumor growth in vitro and in vivo.Acta pharmacologica Sinica · 2021Article
- Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2.Angewandte Chemie (International ed. in English) · 2021Article
- FGFR Inhibitors in Oncology: Insight on the Management of Toxicities in Clinical Practice.Cancers · 2021Review
- Design, synthesis and biological evaluation of pyrazolo[3,4-Acta pharmaceutica Sinica. B · 2021Article
- Novel Regulatory Factors and Small-Molecule Inhibitors of FGFR4 in Cancer.Frontiers in pharmacology · 2021Review
- Rotational Freedom, Steric Hindrance, and Protein Dynamics Explain BLU554 Selectivity for the Hinge Cysteine of FGFR4.ACS medicinal chemistry letters · 2019Article
- Review
- Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening.Journal of the American Chemical Society · 2019Article
Corrections and comments
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Authors and funding
12 authors at 3 institutions in 1 country.
Funding
Abstract
The fibroblast growth factor receptor tyrosine kinases (FGFR1, 2, 3, and 4) represent promising therapeutic targets in a number of cancers. We have developed the first potent and selective irreversible inhibitor of FGFR1, 2, 3, and 4, which we named FIIN-1 that forms a covalent bond with cysteine 486 located in the P loop of the FGFR1 ATP binding site. We demonstrated that the inhibitor potently inhibits Tel-FGFR1-transformed Ba/F3 cells (EC(50) = 14 nM) as well as numerous FGFR-dependent cancer cell lines. A biotin-derivatized version of the inhibitor, FIIN-1-biotin, was shown to covalently label FGFR1 at Cys486. FIIN-1 is a useful probe of FGFR-dependent cellular phenomena and may provide a starting point of the development of therapeutically relevant irreversible inhibitors of wild-type and drug-resistant forms of FGFR kinases.
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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.