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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-364 |
| Subject |
Identification of protein tyrosine phosphatase 1B inhibitors as antidiabetic drugs |
| Authors |
Seung Oh Seo, Sang Jeon Chung1,*
College of Pharmacy, Sungkyunkwan University, Korea
1College of Pharmacy, SungKyunKwan University, Korea
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| Abstract |
Insulin resistance is a key feature of type 2 diabetes and is characterized by downregulation insulin signaling. Protein-Tyrosine Phosphatase 1B (PTP1B) is a negative regulator of the insulin signaling pathways and its increased expression and activity lead to insulin resistance relevant to development of type 2 diabetes. Therefore, PTP1B inhibition is expected to be a potential therapeutic strategy to treat type 2 diabetes. In this study, we investigated whether six natural compounds may have an antidiabetic effect via a PTP1B inhibition. To identify therapeutic candidates for the treatment of type 2 diabetes, six natural compounds were screened for inhibitors of PTP1B relevant to cellular insulin resistance, measuring the enzymatic activity of PTP1B in vitro. Among them, SO48 and SO82 were selected as PTP1B inhibitors and we examined its IC50, Ki value and inhibition type through enzyme kinetics. We also investigated the antidiabetic properties of PTP1B inhibitors in C2C12 muscle cells and 3T3-L1 adipocytes. Our cell-based studies demonstrated that SO48 and SO82 as PTP1B inhibitors could be used as a potential therapeutic candidate for the treatment of type 2 diabetes. |
| E-mail |
wjstkz@naver.com |
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123rd General Meeting of the KCS