Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.

doi:10.1021/acs.jmedchem.5b01082

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

Community

Back to search

Article

Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.

Journal of medicinal chemistry - 10 Sept 2015

Engel Julian, Richters André, Getlik Matthäus, Tomassi Stefano, Keul Marina, Termathe Martin, Lategahn Jonas, Becker Christian, Mayer-Wrangowski Svenja, Grütter Christian, Uhlenbrock Niklas, Krüll Jasmin, Schaumann Niklas, Eppmann Simone, Kibies Patrick, Hoffgaard Franziska, Heil Jochen, Menninger Sascha, Ortiz-Cuaran Sandra, Heuckmann Johannes M, Tinnefeld Verena, Zahedi René P, Sos Martin L, Schultz-Fademrecht Carsten, Thomas Roman K, Kast Stefan M, Rauh Daniel

Abstract excerpt

Receptor tyrosine kinases represent one of the prime targets in cancer therapy, as the dysregulation of these elementary transducers of extracellular signals, like the epidermal growth factor receptor (EGFR), contributes to the onset of cancer, such as non-small cell lung cancer (NSCLC). Strong efforts were directed to the development of irreversible inhibitors and led to compound CO-1686, which takes advantage...

Read the complete abstract on PubMed

Topics

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

Share to Cell Membrane Permeability

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Drug Design

Share to Molecular Conformation

Share to Pyrazoles

Share to Quinazolines

Share to Small Molecule Libraries

Share to Solubility

Share to src-Family Kinases

Source

Open in PubMed

Identifiers

PMID: 26275028
DOI: 10.1021/acs.jmedchem.5b01082

Genes

EGFR

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

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

Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.PMID 26275028Read ↗

Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance.Semantic proximity Read ↗

Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR.Semantic proximity Read ↗

Overcoming Resistance in EGFR-Mutant Cancers: A Comprehensive Review of Inhibitor Evolution and SAR-Based Design.Semantic proximity Read ↗

Structural elements that enable specificity for mutant EGFR kinase domains with next-generation small-molecule inhibitors.Semantic proximity Read ↗

Chemical Scaffolds for the Clinical Development of Mutant-Selective and Reversible Fourth-Generation EGFR-TKIs in NSCLC.Semantic proximity Read ↗

Structure-guided identification and biological evaluation of reversible EGFR C797S inhibitors.Semantic proximity Read ↗

Targeting mutant EGFR in non-small cell lung cancer in the context of cell adaptation and resistanceSemantic proximity Read ↗

Recent Development of the Second and Third Generation Irreversible Epidermal Growth Factor Receptor InhibitorsSemantic proximity Read ↗

Overcoming EGFR resistance by monovalent and bident inhibitors targeting Cys775Semantic proximity Read ↗

Epidermal growth factor receptor as a target enzyme in cancer therapy: Structural and functional insights from crystallography.Semantic proximity Read ↗

Covalent EGFR Inhibitors: Binding Mechanisms, Synthetic Approaches, and Clinical Profiles.Semantic proximity Read ↗

Fighting cancer drug resistance: Opportunities and challenges for mutation-specific EGFR inhibitors.Semantic proximity Read ↗

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