Discover Community Create You

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

Computational biophysical characterization of the effect of gatekeeper mutations on the binding of ponatinib to the FGFR kinase.

Archives of biochemistry and biophysics - 1 Aug 2024

Mahapatra Subhasmita, Kar Parimal

Abstract excerpt

Fibroblast Growth Factor Receptor (FGFR) is connected to numerous downstream signalling cascades regulating cellular behavior. Any dysregulation leads to a plethora of illnesses, including cancer. Therapeutics are available, but drug resistance driven by gatekeeper mutation impedes the treatment. Ponatinib is an FDA-approved drug against BCR-ABL kinase and has shown effective results against FGFR-mediated...

Read the complete abstract on PubMed

Topics

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

Share to Imidazoles
Share to Molecular Dynamics Simulation

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Mutation

Share to Protein Binding

Share to Protein Kinase Inhibitors

Share to Pyridazines

Share to Receptors, Fibroblast Growth Factor

Source

Identifiers

PMID: 38909834
DOI: 10.1016/j.abb.2024.110070

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Computational biophysical characterization of the effect of gatekeeper mutations on the binding of ponatinib to the FGFR kinase.PMID 38909834Read ↗

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

Structural study of ponatinib in inhibiting SRC kinase.Semantic proximity Read ↗

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

Elucidating the potential effects of point mutations on FGFR3 inhibitor resistance via combined molecular dynamics simulation and community network analysis.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 ↗

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

Computational revealing Infigratinib resistance to the FGFR2 N549H and N549K mutationsSemantic proximity Read ↗

Predicting the impact of deleterious mutations in the protein kinase domain of FGFR2 in the context of function, structure, and pathogenesis--a bioinformatics approach.Semantic proximity Read ↗

Structural Analysis of Interactions between Epidermal Growth Factor Receptor (EGFR) Mutants and Their InhibitorsSemantic proximity Read ↗

Structural dynamics and kinase inhibitory activity of three generations of tyrosine kinase inhibitors against wild-type, L858R/T790M, and L858R/T790M/C797S forms of EGFR.Semantic proximity Read ↗

Structural mechanism of the Pan-BCR-ABL inhibitor ponatinib (AP24534): lessons for overcoming kinase inhibitor resistance.Semantic proximity Read ↗

Drug Discovery Using Chemical Systems Biology: Weak Inhibition of Multiple Kinases May Contribute to the Anti-Cancer Effect of NelfinavirSemantic proximity Read ↗

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