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Discovery of novel PDE4 inhibitors targeting the M-pocket from natural mangostanin with improved safety for the treatment of Inflammatory Bowel Diseases.
Author: DengJinhui, HeXixin, HeYue-Ming, HuangYi-You, HuangYue, LiuHaobai, LuoHai-Bin, WangQuan, XieXi, YuanYijun, ZhuJiaqi
Original Abstract of the Article :
Inflammatory Bowel Diseases (IBDs) are chronic disorders with iterative intestinal mucosal inflammation which remain unmet medical needs. PDE4 inhibitors were reported to be novel anti-IBD agents, but their clinical use was hampered by side effects such as emesis and nausea. Herein, structure-based ...See full text at original site
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引用元:
https://doi.org/10.1016/j.ejmech.2022.114631
データ提供:米国国立医学図書館(NLM)
Mangostanin-Derived PDE4 Inhibitors: A New Hope for Inflammatory Bowel Diseases
The search for effective and safe treatments for [inflammatory bowel diseases] (IBD) is an ongoing quest. This study presents a promising new approach utilizing [natural mangostanin] to develop novel and potent [PDE4 inhibitors]. The researchers used a [structure-based drug design] strategy to target the [M-pocket] of [PDE4], a key enzyme involved in the inflammatory process. Their efforts resulted in the identification of a potent and safe [PDE4 inhibitor], [compound 22d], demonstrating the potential of this approach to address the current limitations of existing treatments.
A New Era of Safe and Effective PDE4 Inhibitors
The discovery of [compound 22d] is a significant milestone in the development of [PDE4 inhibitors] for [IBD]. This potent inhibitor, derived from a natural source, exhibits improved safety compared to existing treatments, potentially mitigating the side effects that have hindered their clinical use. The study's findings provide a compelling case for further exploration of [mangostanin] derivatives as a potential source of novel and effective treatments for [IBD].
A More Promising Future for Inflammatory Bowel Diseases
The discovery of [compound 22d] and its promising preclinical results offer hope for a future with more effective and well-tolerated treatments for [IBD]. This research underscores the importance of exploring natural sources for novel drug candidates and highlights the potential of [structure-based drug design] in developing safe and targeted therapies. The ongoing investigation of [mangostanin] derivatives could significantly impact the lives of individuals suffering from [IBD], offering a new avenue for managing this debilitating condition.
Dr. Camel's Conclusion
Just like the desert blooms with unexpected beauty after a rare rainfall, the discovery of mangostanin-derived PDE4 inhibitors offers a glimmer of hope in the fight against inflammatory bowel diseases. This exciting research could bring much-needed relief to patients and pave the way for a brighter future.
Date :
- Date Completed 2022-09-20
- Date Revised 2022-09-20
Further Info :
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