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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Event Hall |
| Time |
4월 19일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-611 |
| Subject |
Investigation of natural compounds for cancer treatment through inhibition of PRL-3 |
| Authors |
Do Hwi Kim, Se Jeong Kwon1, hyo jin kang2, Sang Jeon Chung3,*
Pharmacy, Sungkyunkwan University, Korea
1pharmacy, Sungkyunkwan University, Korea
2Department of Chemistry, Dongguk University, Korea
3Department of Chemistry, SungKyunKwan University, Korea
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| Abstract |
Protein-tyrosine phosphorylation is a reversible posttranslational modification that is essential for eukaryotic cells. The counteracting activities of protein-tyrosine kinases (PTKs) and protein-tyrosine phosphatases (PTPs) regulate the level of cellular tyrosine phosphorylation. Defective or inappropriate operation of these networks leads to aberrant tyrosine phosphorylation, which contributes to the development of many human diseases including cancers, diabetes, and inflammatory disorders.
Phosphatase of regenerating liver-3 (PRL-3) was reported to enhance cell proliferation, motility and invasive activity and to promote cancer metastasis when it was over-expressed. PRL-3 is bound up with cellular process of colorectal, ovarian, prostate and gastric cancers. According to Korea national cancer information center, gastric carcinoma and colorectal cancer was ranked 1st and 2nd sort of high death rate of cancer.
In this study, we have screened 658 natural products purified from traditional oriental medicinal plants and identified inhibitors for PRL-3 with submicromolar Ki values. Furthermore, kinetic evaluation of the potent compounds demonstrates its selectivity and specificity. Therefore, these inhibitors may be an effective lead compound for the development of anticancer drugs.
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| E-mail |
rlaehgnl94@naver.com |
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121st General Meeting of the KCS