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 SreeramuluORCiDGND, Hendrik R. A. JonkerORCiD, Christian RichterORCiDGND, Vladimir V. RogovORCiDGND, Ewgenij ProschakORCiDGND, Bruno Hargittay, Krishna SaxenaORCiDGND, Harald SchwalbeORCiDGND
Parent Title (German):Postprint, zuerst in: Chemistry - A European Journal
Document Type:Article
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
Page Number:5
First Page:7861
Last Page:7865
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
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
Licence (German):License LogoDeutsches Urheberrecht