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

Discovery of novel EGFR-PROTACs capable of degradation of multiple EGFR-mutated proteins.

European journal of medicinal chemistry - 5 Jun 2024

Du Yu, Shi Shi, Shu Chen, He Yezi, Xu Wangyang, Wu Daochen, Tian Yushu, Kong Mingyang, He Jiahuan, Xie Wenhui, Qiu Yijia, Xu Yungen, Zou Yi, Zhu Qihua

Abstract excerpt

Although three generations of Epidermal growth factor receptor (EGFR) - TK inhibitors have been approved for the treatment of Non-small-cell lung cancers (NSCLC), their clinical application is still largely hindered by acquired drug resistance mediated new EGFR mutations and side effects. The Proteolysis targeting chimera (PROTAC) technology has the potential to overcome acquired resistance from mutant EGFR...

Read the complete abstract on PubMed

Topics

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

Share to Dose-Response Relationship, Drug
Share to Drug Discovery

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Drug Screening Assays, Antitumor

Share to Mice, Nude

Share to Molecular Structure

Share to Protein Kinase Inhibitors

Share to Proteolysis

Share to Structure-Activity Relationship

Source

Identifiers

PMID: 38759458
DOI: 10.1016/j.ejmech.2024.116489

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Discovery of novel EGFR-PROTACs capable of degradation of multiple EGFR-mutated proteins.PMID 38759458Read ↗

Design and synthesis of proteolysis targeting chimeras (PROTACs) as an EGFR degrader based on CO-1686.Semantic proximity Read ↗

Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands.Semantic proximity Read ↗

Discovery of highly potent and selective CRBN-recruiting EGFRL858R/T790M degraders in vivo.Semantic proximity Read ↗

Effective degradation of EGFRL858R+T790M mutant proteins by CRBN-based PROTACs through both proteosome and autophagy/lysosome degradation systems.Semantic proximity Read ↗

Targeting EGFR degradation by autophagosome degraders.Semantic proximity Read ↗

Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting C797S Mutation.Semantic proximity Read ↗

Design and synthesis of selective degraders of EGFRL858R/T790M mutant.Semantic proximity Read ↗

Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.Semantic proximity Read ↗

[Research Progress of Proteolysis Targeting Chimeria in NSCLC Therapy].Semantic proximity Read ↗

Proteolysis Targeting Chimera Agents (PROTACs): New Hope for Overcoming the Resistance Mechanisms in Oncogene-Addicted Non-Small Cell Lung CancerSemantic proximity Read ↗

Overcoming Cancer Drug Resistance Utilizing PROTAC TechnologySemantic proximity Read ↗

Cetuximab-based PROteolysis targeting chimera for effectual downregulation of NSCLC with varied EGFR mutations.Semantic proximity Read ↗

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