PUBLICATION

Probing the Effects of the FGFR-Inhibitor Derazantinib on Vascular Development in Zebrafish Embryos

Authors
Kotini, M.P., Bachmann, F., Spickermann, J., McSheehy, P.M., Affolter, M.
ID
ZDB-PUB-210106-27
Date
2020
Source
Pharmaceuticals (Basel, Switzerland)   14(1): (Journal)
Registered Authors
Affolter, Markus
Keywords
FGFR-signalling, VEGFR-signalling, anastomosis, angiogenesis, derazantinib, infigratinib, vascular development, vatalanib, zebrafish
MeSH Terms
none
PubMed
33396726 Full text @ Pharmaceuticals (Basel)
Abstract
Angiogenesis is a fundamental developmental process and a hallmark of cancer progression. Receptor tyrosine kinases (RTK) are targets for cancer therapy which may include their action as anti-angiogenic agents. Derazantinib (DZB) is an inhibitor of the fibroblast growth factor receptors (FGFRs) 1-3 as well as other kinase targets including vascular endothelial growth factor receptor 2 (VEGFR2), colony stimulating factor-1 receptor (CSF1R) and platelet-derived growth factor beta receptor (PDGFRbeta). This study aimed to investigate the effect of DZB on blood vessel morphogenesis and to compare its activity to known specific FGFR and VEGFR inhibitors. For this purpose, we used the developing vasculature in the zebrafish embryo as a model system for angiogenesis in vivo. We show that DZB interferes with multiple angiogenic processes that are linked to FGF and VEGF signalling, revealing a potential dual role for DZB as a potent anti-angiogenic treatment.
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Mutations / Transgenics
Allele Construct Type Affected Genomic Region
hu5333TgTransgenic Insertion
    ncv27TgTransgenic Insertion
      s916TgTransgenic Insertion
        sd2TgTransgenic Insertion
          ubs1TgTransgenic Insertion
            ubs10TgTransgenic Insertion
              y1TgTransgenic Insertion
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                Engineered Foreign Genes
                Marker Marker Type Name
                DsRedEFGDsRed
                EGFPEFGEGFP
                mCherryEFGmCherry
                RFPEFGRFP
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                Citation
                Kotini, M.P., Bachmann, F., Spickermann, J., McSheehy, P.M., Affolter, M. (2020) Probing the Effects of the FGFR-Inhibitor Derazantinib on Vascular Development in Zebrafish Embryos. Pharmaceuticals (Basel, Switzerland). 14(1):.