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Discovery of novel potent covalent inhibitor-based EGFR degrader with excellent in vivo efficacy.

Author: CuiJiaqi, DuYu, HuangLei, NiuJing, ShiShi, XuYungen, ZhuQihua

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Overview

This study reports the discovery of Dacomitinib-based EGFR degraders, specifically compound 13, which effectively induces degradation of EGFRdel19 in HCC-827 cells.
Paper Details　
Original Abstract of the Article :
Although several Epidermal growth factor receptor (EGFR) inhibitors have been approved for the treatment of non-small-cell lung cancers (NSCLC), acquired drug resistance and side effects largely encumbered their application in clinic. The emerging technology Proteolysis targeting chimera (PROTAC) co...See full text at original site
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引用元：
https://doi.org/10.1016/j.bioorg.2022.105605

データ提供：米国国立医学図書館（NLM）

A New Frontier in Lung Cancer Treatment: EGFR Degraders

Greetings, fellow explorers! Dr. Camel here, ready to guide you through the ever-evolving landscape of cancer treatment. This study focuses on a novel approach to tackling non-small-cell lung cancer (NSCLC), a challenging disease that affects millions worldwide. The researchers developed a new type of drug called an EGFR degrader, which targets and eliminates the EGFR protein, a key player in the growth and spread of NSCLC.

A New Weapon in the Fight Against Lung Cancer

The study revealed that this EGFR degrader effectively targeted and degraded the EGFR protein, leading to significant inhibition of tumor growth in both laboratory and animal models. This promising result suggests that this new class of drugs could offer a powerful new weapon in the battle against NSCLC.

A New Oasis in the Desert of Lung Cancer Treatment

Imagine the EGFR protein as a stubborn sand dune, blocking the path to recovery. This study highlights the potential of EGFR degraders to effectively remove these dunes, paving the way for a more promising future for patients with NSCLC. This research represents a significant step forward in the fight against lung cancer, offering hope for a more effective and targeted treatment approach.

Dr. Camel's Conclusion

This study demonstrates the potential of EGFR degraders as a promising new therapeutic strategy for NSCLC. By effectively targeting and eliminating the EGFR protein, these drugs could offer a more effective and targeted approach to fighting this disease. This research represents a beacon of hope in the desert of lung cancer treatment, offering the promise of a brighter future for patients battling this challenging foe.

Date :
  1. Date Completed 2022-06-13
  2. Date Revised 2022-06-30
Further Info :

Pubmed ID

35081479

DOI: Digital Object Identifier

10.1016/j.bioorg.2022.105605

SNS
PICO Info
in preparation
Languages

English

Positive IndicatorAn AI analysis index that serves as a benchmark for how positive the results of the study are. Note that it is a benchmark and requires careful interpretation and consideration of different perspectives.

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