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Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile.

Author: ChenJinju, JiangBiao, KongYing, LiYan, LiuHaixia, QiuXing, RenChaowei, SongXiaoling, SunNing, SunRenhong, YangXiaobao, YinQianqian, ZhangJianshui, ZhongHui, ZhouYuedong

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

Overview

SIAIS164018, a Brigatinib-derived degrader, exhibited unique features, including the ability to degrade ALK fusion proteins and mutant EGFR, key targets in non-small-cell lung cancer. It also inhibited cell migration and invasion and degraded several important oncoproteins involved in metastasis. Importantly, SIAIS164018 was orally bioavailable and well tolerated in vivo.
Paper Details　
Original Abstract of the Article :
Proteolysis-targeting chimera (PROTAC) is an attractive technology in drug discovery. Canonically, targets act as a basic starting point in the most previous PROTAC design. Here, we designed degraders considering from the view of clinical benefits. With this novel design, Brigatinib was turned into ...See full text at original site
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引用元：
https://doi.org/10.1021/acs.jmedchem.1c00373

データ提供：米国国立医学図書館（NLM）

A Revolutionary Approach: Brigatinib Degrader SIAIS164018 Targets Metastasis

Venturing into the vast and challenging landscape of cancer research is like navigating a desert with unpredictable landscapes and hidden oases. This research explores a new approach to cancer treatment, utilizing a protein degrader called SIAIS164018, which targets specific proteins involved in cancer development and metastasis. The study highlights the unique properties of this degrader, emphasizing its potential to effectively destroy cancer cells and inhibit their spread. The authors provide a detailed analysis of the drug's mechanism of action, its impact on various cancer cell lines, and its potential benefits for patients.

A Promising New Tool for Cancer Treatment: The Power of Degraders

The research presents a compelling case for the potential of SIAIS164018 as a novel and effective treatment for cancer. It suggests that this degrader could offer a unique and powerful weapon against both primary tumors and metastatic spread. Like discovering a new and potent elixir in the desert, SIAIS164018 could revolutionize cancer treatment.

Exploring New Frontiers in Cancer Research: The Quest for Effective Therapies

The study highlights the importance of ongoing research and innovation in the pursuit of effective therapies for cancer. It underscores the need for a multidisciplinary approach, involving scientists, clinicians, and patients, to develop new and effective treatments.

Dr.Camel's Conclusion

This research explores the exciting potential of a new protein degrader, SIAIS164018, in the fight against cancer. It offers a glimpse into the future of cancer treatment, where targeted therapies and innovative approaches could significantly impact patient outcomes. Like a camel navigating a vast and challenging desert, researchers continue to seek new solutions to conquer this formidable disease.

Date :
  1. Date Completed 2021-09-07
  2. Date Revised 2021-09-07
Further Info :

Pubmed ID

34138566

DOI: Digital Object Identifier

10.1021/acs.jmedchem.1c00373

Related Literature

Article Analysis
・Effects of brigatinib
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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