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| Type |
Poster Presentation |
| Area |
Life Chemistry |
| Room No. |
Exhibition Hall 2 |
| Time |
4월 19일 (금요일) 11:00~12:30 |
| Code |
LIFE.P-347 |
| Subject |
Antidiabetic effect of CBL through inhibition of protein tyrosine phosphatases relevant to insulin resistance |
| Authors |
Sang Jeon Chung*, Ji Young Hwang1, Do Hee Ahn2, Se Jeong Kwon3
College of Pharmacy, SungKyunKwan University, Korea
1SCHOOL OF PHARMACY, Sungkyunkwan University, Korea
2Pharmacy, Sungkyunkwan University, Korea
3pharmacy, Sungkyunkwan University, Korea
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| Abstract |
We have identified PTPN9 and DUSP9 as potential antidiabetic targets. In this study, PTPN11 knockdown increased AMPK phosphorylation, indicating that PTPN11 could be an antidiabetic target. A library of 658 natural products was screened to identify the inhibitors of PTPN9, DUSP9, or PTPN11. Among the PTP-inhibitory compounds, CBL showed a strong inhibitory activity against PTPN9 and PTPN11, meaning that it would be a potential antidiabetic candidate with a dual targeting of those PTPs. The inhibitory activities of CBL against PTPN9 and PTPN11 were determined to be Ki = 3.4 nM and Ki = 67.4 nM, respectively. Furthermore, CBL stimulated glucose uptake and resulted in increased AMP-activated protein kinase (AMPK) phosphorylation. Taken together, we demonstrated that CBL, as an inhibitor of PTPN9 and PTPN11, increased glucose uptake through activation of the AMPK signaling pathway. These results strongly suggest that CBL could be used as a potential therapeutic candidate for the treatment of type 2 diabetes. |
| E-mail |
genieworld@skku.edu |
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123rd General Meeting of the KCS