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 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 RichterORCiD, Vladimir V. Rogov, Ewgenij ProschakORCiDGND, Bruno Hargittay, Krishna SaxenaORCiDGND, Harald SchwalbeORCiDGND |
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| URN: | urn:nbn:de:hebis:30:3-513172 |
| DOI: | https://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 |
| Page Number: | 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, Chemie und Pharmazie / Biochemie und Chemie |
| Biochemie, Chemie und Pharmazie / Pharmazie | |
| Dewey Decimal Classification: | 5 Naturwissenschaften und Mathematik / 54 Chemie / 540 Chemie und zugeordnete Wissenschaften |
| 5 Naturwissenschaften und Mathematik / 57 Biowissenschaften; Biologie / 570 Biowissenschaften; Biologie | |
| 6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit | |
| Sammlungen: | Universitätspublikationen |
| Licence (German): |  Deutsches Urheberrecht |
