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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.

Author: ChoowongkomonKiattawee, MahalapbutrPanupong, Poo-ArpornRungtiva P, RungrotmongkolThanyada, TodsapornDuangjai

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

Molecular modeling and in vitro studies revealed how EGFR mutations lead to resistance against EGFR tyrosine kinase inhibitors. Osimertinib and afatinib showed better efficacy against mutated EGFRs, guiding the development of new inhibitors.
Paper Details　
Original Abstract of the Article :
Mutations in the tyrosine kinase domain of epidermal growth factor receptor (EGFR), including L858R/T790M double and L858R/T790M/C797S triple mutations, are major causes of acquired resistance towards EGFR targeted drugs. In this work, a combination of comprehensive molecular modeling and in vitro k...See full text at original site
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引用元：
https://doi.org/10.1016/j.compbiomed.2022.105787

データ提供：米国国立医学図書館（NLM）

Tackling Drug Resistance in EGFR-Targeted Cancer Therapies

The battle against cancer is a complex and ever-evolving landscape. One of the major challenges in cancer treatment is drug resistance, where cancer cells develop mechanisms to evade the effects of targeted therapies. This study investigates the effectiveness of three generations of EGFR tyrosine kinase inhibitors (TKIs) against various mutated forms of the EGFR protein, which is a key target in many lung cancers.

Osimertinib: A Promising TKI for Drug-Resistant EGFR Mutations

The researchers found that osimertinib exhibited the strongest inhibitory activity against the mutated forms of EGFR, including the L858R/T790M double mutation and the L858R/T790M/C797S triple mutation. These findings suggest that osimertinib may be a valuable tool for overcoming drug resistance in EGFR-targeted therapies. This is a significant discovery, as it could lead to improved treatment outcomes for patients with drug-resistant lung cancers.

Understanding Drug Resistance Mechanisms for Better Treatment Strategies

This study not only identifies a promising TKI for drug-resistant EGFR mutations but also sheds light on the underlying mechanisms of drug resistance. By understanding these mechanisms, researchers can develop even more effective strategies for overcoming resistance and improving cancer treatment outcomes. It's like finding the hidden springs in the desert – by understanding the water sources, we can overcome the challenges of survival and thrive.

Dr. Camel's Conclusion

This research is like a journey across a vast and unforgiving desert, where every obstacle presents a new challenge. The discovery of osimertinib, a potent TKI, is a beacon of hope in the fight against drug resistance. It's a reminder that with persistence and innovation, we can overcome even the most formidable challenges in the quest for effective cancer therapies.

Date :
  1. Date Completed 2022-07-13
  2. Date Revised 2022-09-16
Further Info :

Pubmed ID

35803080

DOI: Digital Object Identifier

10.1016/j.compbiomed.2022.105787

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in preparation
Languages

English

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