Paralog-specific kinase inhibition of FGFR4: Adding to the arsenal of anti-FGFR agents

Packer, Leisl M. & Pollock, Pamela M. (2015) Paralog-specific kinase inhibition of FGFR4: Adding to the arsenal of anti-FGFR agents. Cancer Discovery, 5(4), pp. 355-357.

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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.

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2 citations in Scopus
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2 citations in Web of Science®

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56 since deposited on 18 May 2015
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ID Code: 84188
Item Type: Journal Article
Refereed: Yes
DOI: 10.1158/2159-8290.CD-15-0246
ISSN: 2159-8290
Divisions: Current > Schools > School of Biomedical Sciences
Current > QUT Faculties and Divisions > Faculty of Health
Current > Institutes > Institute of Health and Biomedical Innovation
Copyright Owner: Copyright 2015 American Association for Cancer Research
Deposited On: 18 May 2015 22:42
Last Modified: 02 May 2016 11:13

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