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 Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.

Journal of medicinal chemistry - 13 Feb 2020

Cheng Meng, Yu Xufen, Lu Kaylene, Xie Ling, Wang Li, Meng Fanye, Han Xiaoran, Chen Xian, Liu Jing, Xiong Yue, Jin Jian

Abstract excerpt

Several epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors have been developed and approved by Food and Drug Administration for the treatment of non-small-cell lung cancers, but their efficacy can be compromised by acquired drug resistance conferred by EGFR-mutant variants. Here, we described the discovery of a novel E3 ligase von Hippel-Lindau-recruiting EGFR degrader, MS39 (compound 6), and a...

Read the complete abstract on PubMed

Topics

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

Share to Adaptor Proteins, Signal Transducing
Share to Drug Design

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Drug Discovery

Share to Gefitinib

Share to Protein Kinase Inhibitors

Share to Proteolysis

Share to Ubiquitin-Protein Ligases

Share to Von Hippel-Lindau Tumor Suppressor Protein

Source

Open in PubMed Open full text

Identifiers

PMID: 31895569
DOI: 10.1021/acs.jmedchem.9b01566
PMCID: PMC7318554

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.PMID 31895569Read ↗

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

Targeted Protein Degradation in Lung Cancer: The Emerging Role of PROTAC Technology and E3 LigasesSemantic proximity Read ↗

Discovery of novel EGFR-PROTACs capable of degradation of multiple EGFR-mutated proteins.Semantic proximity Read ↗

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

Targeting EGFR degradation by autophagosome degraders.Semantic proximity Read ↗

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

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

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

Proteolysis targeting chimeras in non-small cell lung cancer.Semantic proximity Read ↗

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

Clinical Translation of Targeted Protein DegradersSemantic proximity Read ↗

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