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A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.

Author: DuHeliang, GongPing, HuangMin, JingYongkui, WeiYunfei, XieXiaorui, XuQihao, XuYuanbo, ZhaoLinxiang

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Overview

This study investigated a hybrid molecule combining a glycyrrhetinic acid (GA) analogue with Vorinostat (SAHA) to inhibit both HDAC protein and activity. The conjugate (15) of CDODA-Me and SAHA linked through a piperazine group demonstrated potent cytotoxic effects against cancer cells and was more effective than the combination of CDODA-Me and SAHA alone in inducing apoptosis. Compound 15 reduced the levels of HDAC3 and HDAC6 proteins, suggesting a new approach for inhibiting these HDACs.
Paper Details　
Original Abstract of the Article :
Semisynthetic 18β-glycyrrhetinic acid (GA) analogues bearing 1-en-2-cyano-3-oxo substitution on ring A have enhanced antitumor effects with reduced levels of HDAC3 and HDAC6 proteins. Aiming to inhibit both HDAC protein and activity, we developed a hybrid molecule by tethering active GA analogue met...See full text at original site
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引用元：
https://doi.org/10.1016/j.ejmech.2019.111991

データ提供：米国国立医学図書館（NLM）

A Novel HDAC Inhibitor: A Potential Oasis for Cancer Treatment

Cancer, a disease that can feel like a vast and unforgiving desert, has long been a challenge for medical researchers. This study explores the potential of a novel hybrid molecule that combines the strengths of two existing drugs, 18β-glycyrrhetinic acid (GA) and Vorinostat (SAHA), as a new weapon against cancer cells.

A Powerful Alliance: A Hybrid Molecule Shows Promise

The research found that the hybrid molecule, a conjugate of CDODA-Me and SAHA, demonstrated potent cytotoxic activity against cancer cells, leading to apoptosis. This suggests that this hybrid molecule, like a powerful caravan traversing a desert, can effectively target cancer cells, offering a potential oasis of relief in the battle against cancer.

Navigating the Desert: Uncovering the Mechanisms of Action

The study revealed that the hybrid molecule works by reducing the levels of HDAC3 and HDAC6 proteins, key players in the development of cancer. This mechanism of action, like finding a hidden spring in the desert, offers a new and potentially more effective approach to cancer treatment, suggesting that targeting specific proteins involved in cancer growth could lead to more precise and targeted therapies.

Dr. Camel's Conclusion

This study offers a glimmer of hope in the desert of cancer research. The development of this novel hybrid molecule, with its powerful antitumor effects, could offer a new and potentially more effective path to treating cancer. Remember, the journey through the desert of cancer is often challenging, but with innovative approaches and persistent research, a brighter, healthier future is within reach.
Date :
  1. Date Completed 2020-02-17
  2. Date Revised 2020-02-17
Further Info :

Pubmed ID

31883490

DOI: Digital Object Identifier

10.1016/j.ejmech.2019.111991

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・Effects of vorinostat
SNS
PICO Info
in preparation
Languages

English

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