Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

Illuminating the molecular mechanisms of tyrosine kinase inhibitor resistance for the FGFR1 gatekeeper mutation: the Achilles' heel of targeted therapy.

ACS chemical biology - 15 May 2015

Sohl Christal D, Ryan Molly R, Luo BeiBei, Frey Kathleen M, Anderson Karen S

Abstract excerpt

Human fibroblast growth factor receptors (FGFRs) 1-4 are a family of receptor tyrosine kinases that can serve as drivers of tumorigenesis. In particular, FGFR1 gene amplification has been implicated in squamous cell lung and breast cancers. Tyrosine kinase inhibitors (TKIs) targeting FGFR1, including AZD4547 and E3810 (Lucitanib), are currently in early phase clinical trials. Unfortunately, drug resistance limits...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Drug Resistance, Neoplasm
Share to Kinetics

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Models, Molecular

Share to Phosphorylation

Share to Protein Conformation

Share to Protein Kinase Inhibitors

Share to Protein-Tyrosine Kinases

Share to Receptor, Fibroblast Growth Factor, Type 1

Source

Open in PubMed Open full text

Identifiers

PMID: 25686244
DOI: 10.1021/acschembio.5b00014
PMCID: PMC4533833

Genes

FGFR1

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 2 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Illuminating the molecular mechanisms of tyrosine kinase inhibitor resistance for the FGFR1 gatekeeper mutation: the Achilles' heel of targeted therapy.PMID 25686244Read ↗

Gatekeeper mutations activate FGF receptor tyrosine kinases by destabilizing the autoinhibited state.Semantic proximity Read ↗

Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use.Semantic proximity Read ↗

The Effect of Mutations on Drug Sensitivity and Kinase Activity of Fibroblast Growth Factor Receptors: A Combined Experimental and Theoretical StudySemantic proximity Read ↗

DFG-out mode of inhibition by an irreversible type-1 inhibitor capable of overcoming gate-keeper mutations in FGF receptors.Semantic proximity Read ↗

Targeting Gatekeeper Mutations for Kinase Drug DiscoverySemantic proximity Read ↗

Computational biophysical characterization of the effect of gatekeeper mutations on the binding of ponatinib to the FGFR kinase.Semantic proximity Read ↗

The resistance tetrad: amino acid hotspots for kinome-wide exploitation of drug-resistant protein kinase alleles.Semantic proximity Read ↗

Tumour cell responses to new fibroblast growth factor receptor tyrosine kinase inhibitors and identification of a gatekeeper mutation in FGFR3 as a mechanism of acquired resistance.Semantic proximity Read ↗

A general framework for inhibitor resistance in protein kinases.Semantic proximity Read ↗

Computational and Experimental Characterization of Patient Derived Mutations Reveal an Unusual Mode of Regulatory Spine Assembly and Drug Sensitivity in EGFR Kinase.Semantic proximity Read ↗

Saturation mutagenesis identifies activating and resistance-inducing FGFR kinase domain mutations.Semantic proximity Read ↗

The D647N mutation of FGFR1 induces ligand-independent receptor activation.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.