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  • 02월 28일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제123회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Identification of protein tyrosine phosphatase 1B inhibitors as antidiabetic drugs

2019년 2월 13일 11시 15분 00초
LIFE.P-364 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
4월 19일 (금요일) 11:00~12:30
Life Chemistry
저자 및
Seung Oh Seo, Sang Jeon Chung1,*
College of Pharmacy, Sungkyunkwan University, Korea
1College of Pharmacy, SungKyunKwan University, Korea
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.