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Discovery of the Next-Generation Pan-TRK Kinase Inhibitors for the Treatment of Cancer.

Author: DongLin, DuanSijin, GongXiaoyan, LiuZongliang, TianJingwei, WangBingsi, WangHongbo, WangWenyan, YeLiang, YuPengfei

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 identification and optimization of a series of macrocyclic compounds as potent pan-Trk inhibitors. Compound 10 showed good activity against wild and mutant TrkA/TrkC in in vitro and in vivo studies, making it a promising candidate for the treatment of TRK-driven cancers.
Paper Details　
Original Abstract of the Article :
The neurotrophic receptor tyrosine kinase (NTRK) genes including NTRK1, NTRK2, and NTRK3 encode the tropomyosin receptor kinase (Trk) proteins TrkA, TrkB, and TrkC, respectively. So far, two TRK inhibitors, larotrectinib sulfate (LOXO-101 sulfate) and entrectinib (NMS-E628, RXDX-101), have been appr...See full text at original site
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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。

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引用元：
https://doi.org/10.1021/acs.jmedchem.1c00712

データ提供：米国国立医学図書館（NLM）

Pan-TRK Inhibitors: A New Generation of Weapons Against Cancer

This research focuses on the development of next-generation pan-TRK kinase inhibitors, a promising new class of drugs for treating cancers with specific genetic alterations. The study presents the discovery and optimization of a series of macrocyclic compounds as potent pan-TRK inhibitors, demonstrating their effectiveness in inhibiting both wild-type and mutant Trk proteins. These findings offer new possibilities for treating patients with TRK fusion cancers, potentially overcoming resistance to current therapies.

Pan-TRK Inhibitors: A New Arsenal in the Fight Against Cancer

This research highlights the exciting development of pan-TRK kinase inhibitors, a new generation of weapons in the fight against cancer. It's like discovering a hidden arsenal of powerful tools in the vast desert of cancer research, potentially offering a new and more effective approach to treating cancers with specific genetic alterations. The study's findings suggest that pan-TRK inhibitors could become a valuable tool for treating TRK fusion cancers, potentially improving outcomes for patients.

A New Dawn for TRK Fusion Cancer Treatment

This research presents a hopeful outlook for individuals battling TRK fusion cancers. It's like discovering a new and fertile oasis in the desert of cancer research, offering a promising new approach to treatment. The study's findings suggest that pan-TRK inhibitors could revolutionize TRK fusion cancer treatment, potentially leading to more effective therapies and improved outcomes for patients.

Dr. Camel's Conclusion

This research showcases the exciting development of pan-TRK kinase inhibitors, a new generation of weapons in the fight against cancer. It's like discovering a hidden arsenal of powerful tools in the vast desert of cancer research, potentially offering a new and more effective approach to treating cancers with specific genetic alterations. The study's findings are encouraging, potentially leading to more effective and personalized treatment strategies for patients with TRK fusion cancers.

Date :
  1. Date Completed 2021-10-06
  2. Date Revised 2021-10-06
Further Info :

Pubmed ID

34253025

DOI: Digital Object Identifier

10.1021/acs.jmedchem.1c00712

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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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