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NMR backbone assignments of the tyrosine kinase domain of human fibroblast growth factor receptor 3 in apo state and in complex with inhibitor PD173074

Sanfelice, Domenico, Koss, Hans, Bunney, Tom D., Thompson, Gary S., Farrell, Brendan, Katan, Matilda, Breeze, Alexander L. (2018) NMR backbone assignments of the tyrosine kinase domain of human fibroblast growth factor receptor 3 in apo state and in complex with inhibitor PD173074. Biomolecular NMR Assignments, 12 (2). pp. 231-235. ISSN 1874-2718. E-ISSN 1874-270X. (doi:10.1007/s12104-018-9814-7) (KAR id:66867)

Abstract

Fibroblast growth factors receptors (FGFR) are transmembrane protein tyrosine kinases involved in many cellular process,

including growth, differentiation and angiogenesis. Dysregulation of FGFR enzymatic activity is associated with developmental

disorders and cancers; therefore FGFRs have become attractive targets for drug discovery, with a number of agents

in late-stage clinical trials. Here, we present the backbone resonance assignments of FGFR3 tyrosine kinase domain in the

ligand-free form and in complex with the canonical FGFR kinase inhibitor PD173074. Analysis of chemical shift changes

upon inhibitor binding highlights a characteristic pattern of allosteric network perturbations that is of relevance for future

drug discovery activities aimed at development of conformationally-selective FGFR inhibitors.

Item Type: Article
DOI/Identification number: 10.1007/s12104-018-9814-7
Uncontrolled keywords: Fibroblast growth factor receptor 3 Tyrosine kinase inhibitor NMR resonance assignment Cancer Angiogenesis
Divisions: Divisions > Division of Natural Sciences > Biosciences
Depositing User: Gary Thompson
Date Deposited: 30 Apr 2018 09:21 UTC
Last Modified: 28 Jul 2022 22:08 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/66867 (The current URI for this page, for reference purposes)

University of Kent Author Information

Thompson, Gary S..

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