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Discovery of octahydropyrrolo [3,2-b] pyridin derivative as a highly selective Type I inhibitor of FGFR3 over VEGFR2 by high-throughput virtual screening.
Author: ChenGuang-Hui, LiEn-Min, LinWang-Qiang, WangXin, XuLi-Yan, YeCheng-Hao
Original Abstract of the Article :
Although the aberrant activity of fibroblast growth factor receptor 3 (FGFR3) is implicated in various cancers, the reported kinase inhibitors of FGFR3 tend to cause side effects resulting from the inhibitory activity on vascular endothelial growth factor receptor 2 (VEGFR2). Therefore, it is necess...See full text at original site
Dr.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。
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* 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/10.1002/jcb.30357
データ提供:米国国立医学図書館(NLM)
Discovery of a Novel FGFR3 Inhibitor: A Treasure Hunt in the Desert of Drug Discovery
In the expansive desert of drug discovery, where researchers relentlessly search for new treatments, finding a highly selective inhibitor for a specific target is like unearthing a precious gem. This study, like a well-equipped expedition, utilizes high-throughput virtual screening to identify a novel octahydropyrrolo[3,2-b] pyridin derivative that acts as a highly selective type I inhibitor of FGFR3 over VEGFR2. This discovery holds significant promise for developing new cancer therapies.Asinex-5082: A Glimpse of a New Oasis in Cancer Treatment
The study's findings, like a shimmering oasis in the desert, reveal that Asinex-5082, an octahydropyrrolo[3,2-b] pyridin derivative, exhibits remarkable selectivity for FGFR3 over VEGFR2. This discovery, like a map leading to a hidden treasure, could lead to the development of new cancer therapies that target FGFR3 without causing adverse side effects. The study's rigorous approach, using a combination of virtual screening, molecular docking, molecular dynamics simulations, and molecular mechanics Poisson-Boltzmann surface area calculations, provides compelling evidence for the promising potential of Asinex-5082.Navigating the Desert of Cancer Research: A Promise of New Treatments
The implications of this study are far-reaching for the field of cancer research. The discovery of Asinex-5082, like a breakthrough in navigation technology, opens up new avenues for developing more targeted and effective cancer therapies. This research serves as a beacon of hope in the ongoing battle against cancer, offering a glimpse into a future where more selective and effective treatments are available for patients.Dr. Camel's Conclusion
This study's findings, like a refreshing spring in the desert, offer a promising lead in the development of novel FGFR3 inhibitors. The authors, like skilled treasure hunters, have uncovered a valuable compound that could revolutionize cancer treatment. The study's meticulous approach and promising results pave the way for future research and development in this exciting area.Date :
- Date Completed 2023-02-24
- Date Revised 2023-04-02
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