دورية أكاديمية
Ethyl Gallate Dual-Targeting PTPN6 and PPARγ Shows Anti-Diabetic and Anti-Obese Effects
العنوان: | Ethyl Gallate Dual-Targeting PTPN6 and PPARγ Shows Anti-Diabetic and Anti-Obese Effects |
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المؤلفون: | Dohee Ahn, Jinsoo Kim, Gibeom Nam, Xiaodi Zhao, Jihee Kwon, Ji Young Hwang, Jae Kwan Kim, Sun-Young Yoon, Sang J. Chung |
المصدر: | International Journal of Molecular Sciences, Vol 23, Iss 9, p 5020 (2022) |
بيانات النشر: | MDPI AG, 2022. |
سنة النشر: | 2022 |
المجموعة: | LCC:Biology (General) LCC:Chemistry |
مصطلحات موضوعية: | adipogenesis, 3T3-L1 adipocyte, ethyl gallate, natural product, PTPN6, AMPK, Biology (General), QH301-705.5, Chemistry, QD1-999 |
الوصف: | The emergence of the high correlation between type 2 diabetes and obesity with complicated conditions has led to the coinage of the term “diabesity”. AMP-activated protein kinase (AMPK) activators and peroxisome proliferator-activated receptor (PPARγ) antagonists have shown therapeutic activity for diabesity, respectively. Hence, the discovery of compounds that activate AMPK as well as antagonize PPARγ may lead to the discovery of novel therapeutic agents for diabesity. In this study, the knockdown of PTPN6 activated AMPK and suppressed adipogenesis in 3T3-L1 cells. By screening a library of 1033 natural products against PTPN6, we found ethyl gallate to be the most selective inhibitor of PTPN6 (Ki = 3.4 μM). Subsequent assay identified ethyl gallate as the best PPARγ antagonist (IC50 = 5.4 μM) among the hit compounds inhibiting PTPN6. Ethyl gallate upregulated glucose uptake and downregulated adipogenesis in 3T3-L1 cells as anticipated. These results strongly suggest that ethyl gallate, which targets both PTPN6 and PPARγ, is a potent therapeutic candidate to combat diabesity. |
نوع الوثيقة: | article |
وصف الملف: | electronic resource |
اللغة: | English |
تدمد: | 1422-0067 1661-6596 |
Relation: | https://www.mdpi.com/1422-0067/23/9/5020; https://doaj.org/toc/1661-6596; https://doaj.org/toc/1422-0067 |
DOI: | 10.3390/ijms23095020 |
URL الوصول: | https://doaj.org/article/3091b80d9f254d57af370858ea818e9a |
رقم الأكسشن: | edsdoj.3091b80d9f254d57af370858ea818e9a |
قاعدة البيانات: | Directory of Open Access Journals |
تدمد: | 14220067 16616596 |
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DOI: | 10.3390/ijms23095020 |