检索结果-南通市图书馆

daphnane diterpenoids from Trigonostemon lii and Inhibition Activities Against HIV‑1

Natural Products and Bioprospecting 2020年第1期10卷 37-44页

作者： Cheng-Jian Tan Shi-Fei Li Ning Huang Yu Zhang Ying-Tong Di Yong-Tang Zheng Xiao-Jiang Hao State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of BotanyChinese Academy of SciencesKunming 650204YunnanPeople’s Republic of China Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences Center for Biosafety Mega-ScienceKunming Institute of ZoologyChinese Academy of SciencesKunming 650223YunnanPeople’s Republic of China School of Ethnic Medicine Guizhou Minzu UniversityGuiyang 550025GuizhouPeople’s Republic of China Institute of Molecular Science Shanxi UniversityTaiyuan 030006ShanxiPeople’s Republic of China School of Basic Medical Kunming Medical UniversityKunming 650500YunnanPeople’s Republic of China

Natural products are the important source for the discovery of more potent anti-HIV *** this study,six daphnane diterpenoids including three unreported structures were isolated from Trigonostemon lii,which showed signifcant activities against HIV-1 strains replication in the nanomolar/picomolar ***,these diterpenoids signifcantly inhibited the fusion of H9/HIV-1 IIIB cells with uninfected C8166 cells,with the EC50s from 1.06 to 8.73 ng/mL,and did not show any inhibition activities against HIV-1 reverse ***,all of the diterpenoids shows signifcant inhibitions against T20-resistan HIV-1 strains,PNL4-3gp41(36G)V38E,N42S and pNL4-3gp41(36G)V38A,*** results revealed that the six diterpenoids could be a new type of potential lead candidate as an HIV entry inhibitor,particularly for those infected by T20-resistant variants.

关键词： Trigonostemon lii daphnane diterpenoid Trigonolactone Anti-HIV

来源：

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Discovery of a highly potent and orally available importin-β1 inhibitor that overcomes enzalutamide-resistance in advanced prostate cancer

引用

Acta Pharmaceutica Sinica B 2023年第12期13卷 4934-4944页

作者： Jia-Luo Huang Xue-Long Yan Dong Huang Lu Gan Huahua Gao Run-Zhu Fan Shen Li Fang-Yu Yuan Xinying Zhu Gui-Hua Tang Hong-Wu Chen Junjian Wang Sheng Yin School of Pharmaceutical Sciences Sun Yat-sen UniversityGuangzhou 510006China School of Pharmacy Guizhou Medical UniversityGuian New DistrictGuizhou 550025China School of Medicine University of California DavisSacramentoCA 95817USA

Nuclear transporter importin-β1 is emerging as an attractive target by virtue of its prevalence in many ***,the lack of druggable inhibitors restricts its therapeutic proof of *** the present work,we optimized a natural importin-β1 inhibitor DD1 to afford an improved analog DD1-Br with better tolerability(>25 folds)and oral ***1-Br inhibited the survival of castration-resistant prostate cancer(CRPC)cells with sub-nanomolar potency and completely prevented tumor growth in resistant CRPC models both in monotherapy(0.5 mg/kg)and in enzalutamidecombination *** study revealed that by targeting importin-β1,DD1-Br markedly inhibited the nuclear accumulation of multiple CRPC drivers,particularly AR-V7,a main contributor to enzalutamide resistance,leading to the integral suppression of downstream oncogenic *** study provides a promising lead for CRPC and demonstrates the potential of overcoming drug resistance in advanced CRPC via targeting importin-β1.

关键词： Importin-β1 CRPC Drug discovery Enzalutamide-resistance Natural product Cancer daphnane diterpenoid Nuclear transporter

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

欢迎您,

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

在线全文

请选择保存的检索档案：

请选择收藏分类：

通借通还

欢迎您,

建议与咨询 留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

在线全文

请选择保存的检索档案： 新增检索档案 确定 取消

请选择收藏分类： 新增自定义分类 确定 取消

通借通还

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

请选择保存的检索档案：

请选择收藏分类：