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5-苯基-1,3,4-噻二唑衍生物的合成及含SH2结构域蛋白酪氨酸磷酸酶1(SHP1)抑制活性研究 被引量:1
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作者 于丽杰 冯勃 +6 位作者 王智佳 高立信 张纯 rajendran satheeshkumar 李佳 周宇波 王文龙 《有机化学》 SCIE CAS CSCD 北大核心 2021年第8期3097-3105,共9页
作为细胞信号转导通路的关键节点分子,含SH2结构域蛋白酪氨酸磷酸酶1(SHP1)是潜在的抗肿瘤靶点.已知的SHP1抑制剂屈指可数.设计并合成了11个5-苯基-1,3,4-噻二唑衍生物.活性测试结果表明,部分衍生物对SHP1显示了一定强度的抑制活性.其中... 作为细胞信号转导通路的关键节点分子,含SH2结构域蛋白酪氨酸磷酸酶1(SHP1)是潜在的抗肿瘤靶点.已知的SHP1抑制剂屈指可数.设计并合成了11个5-苯基-1,3,4-噻二唑衍生物.活性测试结果表明,部分衍生物对SHP1显示了一定强度的抑制活性.其中,化合物5b[IC50=(1.33±0.16)μmol/L]对SHP1显示了中等强度的抑制活性,对PTP1B和TCPTP不显示抑制活性,对SHP2显示了2倍的选择性,为发现新型SHP1抑制剂提供了新的骨架类型. 展开更多
关键词 5-苯基-1 3 4-噻二唑衍生物 含SH2结构域蛋白酪氨酸磷酸酶1(SHP1) 抑制剂 构效关系
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Small interfering RNA for cancer treatment:overcoming hurdles in delivery 被引量:22
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作者 Nitin Bharat Charbe Nikhil D.Amnerkar +13 位作者 B.Ramesh Murtaza M.Tambuwala Hamid A.Bakshi Alaa A.A.Aljabali Saurabh C.Khadse rajendran satheeshkumar Saurabh Satija Meenu Metha Dinesh Kumar Chellappan Garima Shrivastava Gaurav Gupta Poonam Negi Kamal Dua Flavia C.Zacconin 《Acta Pharmaceutica Sinica B》 SCIE CAS CSCD 2020年第11期2075-2109,共35页
In many ways,cancer cells are different from healthy cells.A lot of tactical nano-based drug delivery systems are based on the difference between cancer and healthy cells.Currently,nanotechnology-based delivery system... In many ways,cancer cells are different from healthy cells.A lot of tactical nano-based drug delivery systems are based on the difference between cancer and healthy cells.Currently,nanotechnology-based delivery systems are the most promising tool to deliver DNA-based products to cancer cells.This review aims to highlight the latest development in the lipids and polymeric nanocarrier for siRNA delivery to the cancer cells.It also provides the necessary information about siRNA development and its mechanism of action.Overall,this review gives us a clear picture of lipid and polymer-based drug delivery systems,which in the future could form the base to translate the basic siRNA biology into siRNA-based cancer therapies. 展开更多
关键词 Small interfering RNA(siRNA) NANOMEDICINE Liposomes Micelles CANCER POLYMER
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