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Structure–Activity Relationship of Synthetic Ginkgolic Acid Analogs for Treating Type 2 Diabetes by PTPN9 Inhibition

التفاصيل البيبلوغرافية
العنوان: Structure–Activity Relationship of Synthetic Ginkgolic Acid Analogs for Treating Type 2 Diabetes by PTPN9 Inhibition
المؤلفون: Jinsoo Kim, Jinyoung Son, Dohee Ahn, Gibeom Nam, Xiaodi Zhao, Hyuna Park, Woojoo Jeong, Sang J. Chung
المصدر: International Journal of Molecular Sciences, Vol 23, Iss 7, p 3927 (2022)
بيانات النشر: MDPI AG, 2022.
سنة النشر: 2022
المجموعة: LCC:Biology (General)
LCC:Chemistry
مصطلحات موضوعية: ginkgolic acid analogs, PTPN9 inhibitors, glucose uptake, insulin sensitivity, AMPK, Akt, Biology (General), QH301-705.5, Chemistry, QD1-999
الوصف: Ginkgolic acid (C13:0) (GA), isolated from Ginkgo biloba, is a potential therapeutic agent for type 2 diabetes. A series of GA analogs were designed and synthesized for the evaluation of their structure–activity relationship with respect to their antidiabetic effects. Unlike GA, the synthetic analog 1e exhibited improved inhibitory activity against PTPN9 and significantly stimulated glucose uptake via AMPK phosphorylation in differentiated 3T3-L1 adipocytes and C2C12 myotubes; it also induced insulin-dependent AKT activation in C2C12 myotubes in a concentration-dependent manner. Docking simulation results showed that 1e had a better binding affinity through a unique hydrophobic interaction with a PTPN9 hydrophobic groove. Moreover, 1e ameliorated palmitate-induced insulin resistance in C2C12 cells. This study showed that 1e increases glucose uptake and suppresses palmitate-induced insulin resistance in C2C12 myotubes via PTPN9 inhibition; thus, it is a promising therapeutic candidate for treating type 2 diabetes.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 1422-0067
1661-6596
Relation: https://www.mdpi.com/1422-0067/23/7/3927; https://doaj.org/toc/1661-6596; https://doaj.org/toc/1422-0067
DOI: 10.3390/ijms23073927
URL الوصول: https://doaj.org/article/05324d9ae0464a148ce0f8cd9867d6f5
رقم الأكسشن: edsdoj.05324d9ae0464a148ce0f8cd9867d6f5
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:14220067
16616596
DOI:10.3390/ijms23073927