Shp2 protein tyrosine phosphatase inhibitor activity of estramustine phosphate and its triterpenoid analogs.
Shp2 protein tyrosine phosphatase inhibitor activity of estramustine phosphate and its triterpenoid analogs.
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DOI：
10.1016/j.bmcl.2010.11.117
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发表时间：
2011-01-15
影响因子：
2.7
通讯作者：
Wu, Jie
中科院分区：
文献类型：
--
作者：
Scott, Latanya M.;Chen, Liwei;Daniel, Kenyon G.;Brooks, Wesley H.;Guida, Wayne C.;Lawrence, Harshani R.;Sebti, Said M.;Lawrence, Nicholas J.;Wu, Jie
Shp2 protein tyrosine phosphate (PTP) is a novel target for anticancer drug discovery. We identified estramustine phosphate as a Shp2 PTP inhibitor from the National Cancer Institute Approved Oncology Drug set. A focused structure-activity relationship study indicated that the 17- phosphate group is required for the Shp2 PTP inhibitor activity of estramustine phosphate. A search for estramustine phosphate analogs led to identification of two triperpenoids, enoxolone and celastrol, having Shp2 PTP inhibitor activity. With the previously reported PTP1B inhibitor trodusquemine, our study reveals steroids and triterpenoids with negatively charged phosphate, carboxylate, or sulfonate groups as novel pharmacophores of selective PTP inhibitors.
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影响因子：
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通讯作者：
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影响因子：
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2.7
作者：
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通讯作者：
BLICKENSTAFF, RT