Intrinsic fluorescence of the clinically approved multikinase inhibitor nintedanib reveals lysosomal sequestration as resistance mechanism in FGFR-driven lung cancer.
Identifieur interne : 000D10 ( Main/Exploration ); précédent : 000D09; suivant : 000D11Intrinsic fluorescence of the clinically approved multikinase inhibitor nintedanib reveals lysosomal sequestration as resistance mechanism in FGFR-driven lung cancer.
Auteurs : Bernhard Englinger [Autriche] ; Sebastian Kallus [Autriche] ; Julia Senkiv [Autriche] ; Daniela Heilos [Autriche] ; Lisa Gabler [Autriche] ; Sushilla Van Schoonhoven [Autriche] ; Alessio Terenzi [Autriche] ; Patrick Moser [Autriche] ; Christine Pirker [Autriche] ; Gerald Timelthaler [Autriche] ; Walter J Ger [Autriche] ; Christian R. Kowol [Autriche] ; Petra Heffeter [Autriche] ; Michael Grusch [Autriche] ; Walter Berger [Autriche]Source :
- Journal of experimental & clinical cancer research : CR [ 1756-9966 ] ; 2017.
Descripteurs français
- KwdFr :
- Animaux, Fluorescence, Humains, Indoles (administration et posologie), Indoles (pharmacocinétique), Lignée cellulaire tumorale, Lysosomes (), Lysosomes (métabolisme), Macrolides (administration et posologie), Phosphorylation (), Poumon (), Poumon (anatomopathologie), Prolifération cellulaire (), Protocoles de polychimiothérapie antinéoplasique (administration et posologie), Récepteur facteur croissance fibroblaste (antagonistes et inhibiteurs), Récepteur facteur croissance fibroblaste (génétique), Souris, Synergie des médicaments, Tests d'activité antitumorale sur modèle de xénogreffe, Transduction du signal (), Tumeurs du poumon (anatomopathologie), Tumeurs du poumon (génétique), Tumeurs du poumon (traitement médicamenteux).
- MESH :
- administration et posologie : Indoles, Macrolides, Protocoles de polychimiothérapie antinéoplasique.
- anatomopathologie : Poumon, Tumeurs du poumon.
- antagonistes et inhibiteurs : Récepteur facteur croissance fibroblaste.
- génétique : Récepteur facteur croissance fibroblaste, Tumeurs du poumon.
- métabolisme : Lysosomes.
- pharmacocinétique : Indoles.
- traitement médicamenteux : Tumeurs du poumon.
- Animaux, Fluorescence, Humains, Lignée cellulaire tumorale, Lysosomes, Phosphorylation, Poumon, Prolifération cellulaire, Souris, Synergie des médicaments, Tests d'activité antitumorale sur modèle de xénogreffe, Transduction du signal.
English descriptors
- KwdEn :
- Animals, Antineoplastic Combined Chemotherapy Protocols (administration & dosage), Cell Line, Tumor, Cell Proliferation (drug effects), Drug Synergism, Fluorescence, Humans, Indoles (administration & dosage), Indoles (pharmacokinetics), Lung (drug effects), Lung (pathology), Lung Neoplasms (drug therapy), Lung Neoplasms (genetics), Lung Neoplasms (pathology), Lysosomes (drug effects), Lysosomes (metabolism), Macrolides (administration & dosage), Mice, Phosphorylation (drug effects), Receptors, Fibroblast Growth Factor (antagonists & inhibitors), Receptors, Fibroblast Growth Factor (genetics), Signal Transduction (drug effects), Xenograft Model Antitumor Assays.
- MESH :
- chemical , administration & dosage : Indoles, Macrolides.
- administration & dosage : Antineoplastic Combined Chemotherapy Protocols.
- chemical , antagonists & inhibitors : Receptors, Fibroblast Growth Factor.
- drug effects : Cell Proliferation, Lung, Lysosomes, Phosphorylation, Signal Transduction.
- drug therapy : Lung Neoplasms.
- genetics : Lung Neoplasms, Receptors, Fibroblast Growth Factor.
- metabolism : Lysosomes.
- pathology : Lung, Lung Neoplasms.
- chemical , pharmacokinetics : Indoles.
- Animals, Cell Line, Tumor, Drug Synergism, Fluorescence, Humans, Mice, Xenograft Model Antitumor Assays.
Abstract
Studying the intracellular distribution of pharmacological agents, including anticancer compounds, is of central importance in biomedical research. It constitutes a prerequisite for a better understanding of the molecular mechanisms underlying drug action and resistance development. Hyperactivated fibroblast growth factor receptors (FGFRs) constitute a promising therapy target in several types of malignancies including lung cancer. The clinically approved small-molecule FGFR inhibitor nintedanib exerts strong cytotoxicity in FGFR-driven lung cancer cells. However, subcellular pharmacokinetics of this compound and its impact on therapeutic efficacy remain obscure.
DOI: 10.1186/s13046-017-0592-3
PubMed: 28882160
Affiliations:
Links toward previous steps (curation, corpus...)
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Le document en format XML
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<author><name sortKey="Grusch, Michael" sort="Grusch, Michael" uniqKey="Grusch M" first="Michael" last="Grusch">Michael Grusch</name>
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<author><name sortKey="Berger, Walter" sort="Berger, Walter" uniqKey="Berger W" first="Walter" last="Berger">Walter Berger</name>
<affiliation wicri:level="3"><nlm:affiliation>Institute of Cancer Research and Comprehensive Cancer Center, Department of Medicine I, Medical University of Vienna, Borschkegasse 8a, A-1090, Vienna, Austria. walter.berger@meduniwien.ac.at.</nlm:affiliation>
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<series><title level="j">Journal of experimental & clinical cancer research : CR</title>
<idno type="eISSN">1756-9966</idno>
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<term>Receptors, Fibroblast Growth Factor (antagonists & inhibitors)</term>
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<term>Signal Transduction (drug effects)</term>
<term>Xenograft Model Antitumor Assays</term>
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<front><div type="abstract" xml:lang="en">Studying the intracellular distribution of pharmacological agents, including anticancer compounds, is of central importance in biomedical research. It constitutes a prerequisite for a better understanding of the molecular mechanisms underlying drug action and resistance development. Hyperactivated fibroblast growth factor receptors (FGFRs) constitute a promising therapy target in several types of malignancies including lung cancer. The clinically approved small-molecule FGFR inhibitor nintedanib exerts strong cytotoxicity in FGFR-driven lung cancer cells. However, subcellular pharmacokinetics of this compound and its impact on therapeutic efficacy remain obscure.</div>
</front>
</TEI>
<affiliations><list><country><li>Autriche</li>
</country>
<region><li>Vienne (Autriche)</li>
</region>
<settlement><li>Vienne (Autriche)</li>
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</list>
<tree><country name="Autriche"><region name="Vienne (Autriche)"><name sortKey="Englinger, Bernhard" sort="Englinger, Bernhard" uniqKey="Englinger B" first="Bernhard" last="Englinger">Bernhard Englinger</name>
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<name sortKey="Berger, Walter" sort="Berger, Walter" uniqKey="Berger W" first="Walter" last="Berger">Walter Berger</name>
<name sortKey="Gabler, Lisa" sort="Gabler, Lisa" uniqKey="Gabler L" first="Lisa" last="Gabler">Lisa Gabler</name>
<name sortKey="Grusch, Michael" sort="Grusch, Michael" uniqKey="Grusch M" first="Michael" last="Grusch">Michael Grusch</name>
<name sortKey="Heffeter, Petra" sort="Heffeter, Petra" uniqKey="Heffeter P" first="Petra" last="Heffeter">Petra Heffeter</name>
<name sortKey="Heilos, Daniela" sort="Heilos, Daniela" uniqKey="Heilos D" first="Daniela" last="Heilos">Daniela Heilos</name>
<name sortKey="J Ger, Walter" sort="J Ger, Walter" uniqKey="J Ger W" first="Walter" last="J Ger">Walter J Ger</name>
<name sortKey="Kallus, Sebastian" sort="Kallus, Sebastian" uniqKey="Kallus S" first="Sebastian" last="Kallus">Sebastian Kallus</name>
<name sortKey="Kowol, Christian R" sort="Kowol, Christian R" uniqKey="Kowol C" first="Christian R" last="Kowol">Christian R. Kowol</name>
<name sortKey="Moser, Patrick" sort="Moser, Patrick" uniqKey="Moser P" first="Patrick" last="Moser">Patrick Moser</name>
<name sortKey="Pirker, Christine" sort="Pirker, Christine" uniqKey="Pirker C" first="Christine" last="Pirker">Christine Pirker</name>
<name sortKey="Senkiv, Julia" sort="Senkiv, Julia" uniqKey="Senkiv J" first="Julia" last="Senkiv">Julia Senkiv</name>
<name sortKey="Terenzi, Alessio" sort="Terenzi, Alessio" uniqKey="Terenzi A" first="Alessio" last="Terenzi">Alessio Terenzi</name>
<name sortKey="Timelthaler, Gerald" sort="Timelthaler, Gerald" uniqKey="Timelthaler G" first="Gerald" last="Timelthaler">Gerald Timelthaler</name>
<name sortKey="Van Schoonhoven, Sushilla" sort="Van Schoonhoven, Sushilla" uniqKey="Van Schoonhoven S" first="Sushilla" last="Van Schoonhoven">Sushilla Van Schoonhoven</name>
</country>
</tree>
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</record>
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