Structural characterization of the interaction of the fibroblast growth factor receptor with a small molecule allosteric inhibitor

The interaction of fibroblast growth factors (FGFs) with their fibroblast growth factor receptors (FGFRs) are important in the signaling network of cell growth and development. SSR128129E (SSR),[1, 2] a ligand of small m
The interaction of fibroblast growth factors (FGFs) with their fibroblast growth factor receptors (FGFRs) are important in the signaling network of cell growth and development. SSR128129E (SSR),[1, 2] a ligand of small molecular weight with potential anti-cancer properties, acts allosterically on the extracellular domains of FGFRs. Up to now, the structural basis of SSR binding to the D3 domain of FGFR remained elusive. This work reports the structural characterization of the interaction of SSR with one specific receptor, FGFR3, by NMR spectroscopy. This information provides a basis for rational drug design for allosteric FGFR inhibitors.
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Author:Franziska Kappert, Sridhar Sreeramulu, Hendrik R. A. Jonker, Christian Richter, Vladimir V. Rogov, Ewgenij Proschak, Bruno Hargittay, Krishna Saxena, Harald Schwalbe
URN:urn:nbn:de:hebis:30:3-513172
DOI:http://dx.doi.org/10.1002/chem.201801770
Parent Title (German):Postprint, zuerst in: Chemistry - A European Journal
Document Type:Article
Language:English
Year of Completion:2019
Date of first Publication:2018/04/14
Publishing Institution:Universitätsbibliothek Johann Christian Senckenberg
Release Date:2019/09/21
Tag:FGFR; NMR Spectroscopy; SSR128129E; allostery; inhibitor
Volume:24
Issue:31
Pagenumber:5
First Page:7861
Last Page:7865
Note:
Postprint, zuerst in: Chemistry - A European Journal 24.2018, 31, S. 7861-7865, doi: 10.1002/chem.201801770
Gefördert durch: European Union: Horizon 2020. Infrastructure for NMR, EM and X-rays for Translational Research, iNEXT, H2020 Grant # 653706
HeBIS PPN:454004001
Institutes:Biochemie und Chemie
Pharmazie
Dewey Decimal Classification:540 Chemie und zugeordnete Wissenschaften
570 Biowissenschaften; Biologie
610 Medizin und Gesundheit
Sammlungen:Universitätspublikationen
Licence (German):License LogoDeutsches Urheberrecht

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