Understanding the mechanism of action of pyrrolo[3,2-b]quinoxaline-derivatives as kinase inhibitors
Abstract: The X-ray structure of the catalytic domain of the EphA3 tyrosine kinase in complex with a previously reported type II inhibitor was used to design two novel quinoxaline derivatives, inspired by kinase inhibitors that have reached clinical development. These two new compounds were characterized by an array of cell-based assays and gene expression profiling experiments. A global chemical proteomics approach was used to generate the drug-protein interaction profile, which suggested suitable therapeutic indications. Both inhibitors, studied in the context of angiogenesis and in vivo in a relevant lymphoma model, showed high efficacy in the control of tumor size
- Sprache
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Englisch
- Umfang
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Online-Ressource
- Anmerkungen
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RSC medicinal chemistry. - 11, 6 (2020) , 665-675, ISSN: 2040-2511
- Standort
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Deutsche Nationalbibliothek Frankfurt am Main
- Urheber
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Unzue, Andrea
Jessen-Trefzer, Claudia
Spiliotopoulos, Dimitrios
Gaudio, Eugenio
Tarantelli, Chiara
Dong, Jing
Zhao, Hongtao
Pachmayr, Johanna
Zahler, Stefan
Bernasconi, Elena
Sartori, Giulio
Cascione, Luciano
Bertoni, Francesco
Śledź, Paweł
Caflisch, Amedeo
Nevado Blázquez, Cristina
- Ereignis
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Veröffentlichung
- (wo)
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Freiburg
- (wer)
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Universität
- (wann)
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2020
- DOI
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10.1039/D0MD00049C
- URN
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urn:nbn:de:bsz:25-freidok-1665457
- Rechteinformation
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Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Letzte Aktualisierung
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25.03.2025, 13:45 MEZ
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Beteiligte
- Unzue, Andrea
- Jessen-Trefzer, Claudia
- Spiliotopoulos, Dimitrios
- Gaudio, Eugenio
- Tarantelli, Chiara
- Dong, Jing
- Zhao, Hongtao
- Pachmayr, Johanna
- Zahler, Stefan
- Bernasconi, Elena
- Sartori, Giulio
- Cascione, Luciano
- Bertoni, Francesco
- Śledź, Paweł
- Caflisch, Amedeo
- Nevado Blázquez, Cristina
- Universität
Entstanden
- 2020
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