TY  - JOUR
A1  - Kappert, Franziska
A1  - Sreeramulu, Sridhar
A1  - Jonker, Hendrik R. A.
A1  - Richter, Christian
A1  - Rogov, Vladimir V.
A1  - Proschak, Ewgenij
A1  - Hargittay, Bruno
A1  - Saxena, Krishna
A1  - Schwalbe, Harald
T1  - Structural characterization of the interaction of the fibroblast growth factor receptor with a small molecule allosteric inhibitor
T2  - Postprint, zuerst in: Chemistry - A European Journal
N2  - 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.
KW  - allostery
KW  - FGFR
KW  - inhibitor
KW  - NMR Spectroscopy
KW  - SSR128129E
Y1  - 2018
UR  - http://publikationen.ub.uni-frankfurt.de/frontdoor/index/index/docId/51317
UR  - https://nbn-resolving.org/urn:nbn:de:hebis:30:3-513172
N1  - 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
VL  - 24
IS  - 31
SP  - 7861
EP  - 7865
ER  -