title: Paralog-Specific Kinase Inhibition of FGFR4: Adding to the Arsenal of Anti-FGFR Agents.
abstract: In this issue of Cancer Discovery, Hagel and colleagues report the design and the in vitro and in vivo activity of a novel, irreversible, paralog-specific kinase inhibitor of FGFR4, BLU9931. This compound binds covalently to a cysteine residue in the hinge region of FGFR4 but not in FGFR1-3. BLU9931 induces tumor shrinkage in hepatocellular carcinoma models that express a functioning ligand/receptor complex consisting of FGF19/FGFR4/KLB and adds to a growing list of anti-FGFR4 agents.
authors.affiliation: Institute of Health and Biomedical Innovation, School of Biomedical Sciences, Queensland University of Technology, Brisbane, Australia.
authors.forename: Leisl M
authors.initials: LM
authors.lastname: Packer
authors.affiliation: Institute of Health and Biomedical Innovation, School of Biomedical Sciences, Queensland University of Technology, Brisbane, Australia. pamela.pollock@qut.edu.au.
authors.forename: Pamela M
authors.initials: PM
authors.lastname: Pollock
mesh_terms: D000818:Animals; D006528:Carcinoma, Hepatocellular / Q000378:metabolism*; D006801:Humans; D008113:Liver Neoplasms / Q000378:metabolism*; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D051499:Receptor, Fibroblast Growth Factor, Type 4 / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects*
chemical_list: D047428:Protein Kinase Inhibitors; D051499:Receptor, Fibroblast Growth Factor, Type 4