Paper Details

  1. Home
  2. Paper Details

Discovery and optimization of selective RET inhibitors via scaffold hopping.

Author: ChenJian, ChenShuhui, FuZhifei, HuGuoping, LiJian, LuoMiaorong, LuoZhibo, ShuaiBin, SunJikui, WangJiansong, WangLingli, ZhangYang

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 focuses on the development of novel RET inhibitors for treating RET-rearranged cancers, such as thyroid and lung cancer. The researchers identified a promising compound, compound 9, which exhibits high potency and selectivity for RET while demonstrating fewer off-target effects compared to existing inhibitors.
Paper Details　
Original Abstract of the Article :
Aberrant alterations of rearranged during transfection (RET) have been identified as actionable drivers of multiple cancers, including thyroid carcinoma and lung cancer. Currently, several approved multikinase inhibitors such as vandetanib and cabozantinib demonstrate clinical activity in patients w...See full text at original site
Dr.Camel IconDr.Camel's Paper Summary Blogラクダ博士について

ラクダ博士は、Health Journal が論文の内容を分かりやすく解説するために作成した架空のキャラクターです。
難解な医学論文を、専門知識のない方にも理解しやすいように、噛み砕いて説明することを目指しています。

* ラクダ博士による解説は、あくまで論文の要点をまとめたものであり、原論文の完全な代替となるものではありません。詳細な内容については、必ず原論文をご参照ください。
* ラクダ博士は架空のキャラクターであり、実際の医学研究者や医療従事者とは一切関係がありません。
* 解説の内容は Health Journal が独自に解釈・作成したものであり、原論文の著者または出版社の見解を反映するものではありません。


引用元：
https://doi.org/10.1016/j.bmcl.2021.128149

データ提供：米国国立医学図書館（NLM）

Selective RET Inhibitors: Targeting Cancer with Precision

This research delves into the development of selective rearranged during transfection (RET) inhibitors, promising therapeutic agents for cancers driven by RET alterations. The researchers designed and synthesized a series of RET inhibitors based on the structure of BLU-667, aiming to improve potency and selectivity. The study identified compound 9 as a novel, potent, and selective RET inhibitor with enhanced drug-like properties, demonstrating its potential for targeted cancer therapy.

A New Era of Targeted Cancer Therapy

The discovery of compound 9, a highly selective RET inhibitor, marks a significant step towards personalized cancer therapy. By precisely targeting RET alterations, this compound offers a potential strategy for effectively treating cancers driven by these specific mutations, while minimizing off-target effects.

The Future of Cancer Treatment: Precision and Personalized Medicine

This research exemplifies the ongoing advancements in precision medicine, where treatments are tailored to the individual's unique genetic makeup. The development of selective RET inhibitors represents a significant shift towards personalized cancer therapy, offering hope for improved treatment outcomes and reduced side effects.

Dr.Camel's Conclusion

The desert of cancer research is vast, and the search for effective treatments can feel like a relentless journey. This research, like a shimmering oasis in the midst of this challenging landscape, offers a glimmer of hope. The development of selective RET inhibitors represents a promising step towards targeted cancer therapy, paving the way for a more personalized and effective approach to treating this devastating disease.

Date :
  1. Date Completed 2022-01-04
  2. Date Revised 2022-01-04
Further Info :

Pubmed ID

34058344

DOI: Digital Object Identifier

10.1016/j.bmcl.2021.128149

Related Literature

Article Analysis
・Effects of cabozantinib (thyroid cancer)
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.

This site uses cookies. Visit our privacy policy page or click the link in any footer for more information and to change your preferences.