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Serendipitous discovery of Class I HDAC inhibitors from rational design of molecular glue degraders targeting HDAC.
Author: AnJianxiong, ChenDi, ChenLei, GuZhicheng, HeBin, LinShuxian, YanWanli, ZengZiwei
Original Abstract of the Article :
Zinc-dependent histone deacetylases (HDACs) play an essential role as epigenetic regulators and are becoming increasingly important drug targets for the treatment of cancer. Although five HDAC inhibitors have been approved for treating several cancers, only one of them is a Class I HDAC inhibitor, w...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。
* 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.ejmech.2023.115926
データ提供:米国国立医学図書館(NLM)
A Serendipitous Discovery in Cancer Treatment: New HDAC Inhibitors
In the realm of cancer research, scientists are constantly seeking novel weapons to combat this deadly disease. This study takes us on an exciting journey through the world of epigenetic regulators, specifically histone deacetylases (HDACs). The team started with the goal of creating molecular glue degraders, compounds that would target HDACs for destruction, but stumbled upon a serendipitous discovery—two new compounds (2f and 3f) that act as potent inhibitors of Class I HDACs. These compounds displayed selective activity against Class I HDACs in cancer cells, exhibiting antiproliferative effects comparable to the approved drug Chidamide.
Promising Candidates for Cancer Treatment
The discovery of compounds 2f and 3f as selective Class I HDAC inhibitors offers a beacon of hope in the fight against cancer. The team observed robust antiproliferative activity against various hematological tumor cells, suggesting a promising therapeutic potential for these compounds. These findings open new avenues for developing targeted therapies that specifically inhibit Class I HDACs.
A Glimpse into the Future of Cancer Treatment
The discovery of selective Class I HDAC inhibitors like compounds 2f and 3f is a promising development in the field of cancer therapy. It represents a step towards personalized medicine, where treatments can be tailored to specific molecular targets within cancer cells. Further research is needed to explore the clinical potential of these compounds, but this discovery certainly invigorates the quest for new and effective therapies for cancer.
Dr.Camel's Conclusion
This research is like finding a hidden oasis in the vast desert of cancer research. The serendipitous discovery of these new HDAC inhibitors, which target specific types of HDACs, is a significant leap forward. It opens new doors for developing more targeted and effective therapies for cancer, offering a hopeful outlook for patients battling this disease.
Date :
- Date Completed 2023-12-04
- Date Revised 2023-12-04
Further Info :
Related Literature
English
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