Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: Comparison of binding to non-phosphorylated and phosphorylated VEGFR2
- Author
- IWATA, Hidehisa1 ; IMAMURA, Shinichi2 ; HORI, Akira2 ; HIXON, Mark S3 ; KIMURA, Hiroyuki1 ; MIKI, Hiroshi1
[1] Discovery Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company Ltd, 26-1, Muraoka-Higashi, 2-chome, Fujisawa, Kanagawa 251-8555, Japan
[2] Oncology Drug Discovery Unit, Pharmaceutical Research Division, Takeda Pharmaceutical Company Ltd, 26-1, Muraoka-Higashi, 2-chome, Fujisawa, Kanagawa 251-8555, Japan
[3] Takeda San Diego Inc., 10410 Science Center Drive, San Diego, CA 92121, United States - Source
Bioorganic & medicinal chemistry. 2011, Vol 19, Num 18, pp 5342-5351, 10 p ; ref : 34 ref
- ISSN
- 0968-0896
- Scientific domain
- Biochemistry, molecular biology, biophysics; Pharmacology drugs
- Publisher
- Elsevier, Amsterdam
- Publication country
- Netherlands
- Document type
- Article
- Language
- English
- Author keyword
- Phosphorylation Slow binding mechanism Type-II inhibitor Vascular endothelial growth factor receptor 2
- Keyword (fr)
- Activité biologique Alcaloïde Antiangiogénique Anticancéreux Autophosphorylation Cinétique Etude comparative Facteur angiogène Facteur croissance endothélium vasculaire Fluor Composé organique In vitro Inhibiteur enzyme Mécanisme action Phosphorylation Récepteur facteur croissance Résonance plasmon surface Sorafénib Sunitinib Transduction signal Transferases Urées Inhibiteur VEGFR2 Pyrrolo[3,2-d]pyrimidine dérivé Pyrrolopyrimidine Receptor protein-tyrosine kinase Staurosporine dérivé Urée(1-[2-fluoro-4-(pyrrolo[3,2-d]pyrimidin-4-yloxy)phényl]-3-[3-trifluorométhylphényl]) VEGFR2 Enzyme
- Keyword (en)
- Biological activity Alkaloid Antiangiogenic agent Antineoplastic agent Autophosphorylation Kinetics Comparative study Angiogenic factor Vascular endothelium growth factor Fluorine Organic compounds In vitro Enzyme inhibitor Mechanism of action Phosphorylation Growth factor receptor Surface plasmon resonance Sorafenib Sunitinib Signal transduction Transferases Ureas Receptor protein-tyrosine kinase Enzyme
- Keyword (es)
- Actividad biológica Alcaloide Antiangiogenico Anticanceroso Autofosforilación Cinética Estudio comparativo Factor angiógeno Factor crecimiento endotelio vascular Fluor Compuesto orgánico In vitro Inhibidor enzima Mecanismo acción Fosforilación Receptor factor crecimiento Sorafenib Sunitinib Transducción señal Transferases Ureas Receptor protein-tyrosine kinase Enzima
- Classification
- Pascal
- 002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments / 002B02R Antineoplastic agents / 002B02R01 General aspects
- Discipline
- Pharmacological treatments
- Origin
- Inist-CNRS
- Database
- PASCAL
- INIST identifier
- 24607858
Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS
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DOI
10.1016/j.bmc.2011.08.002 
https://dx.doi.org/10.1016/j.bmc.2011.08.002
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