Reprogramming Energy Metabolism with Synthesized PDK Inhibitors Based on Dichloroacetate Derivatives and Targeted Delivery Systems for Enhanced Cancer Therapy

首页 > 成果 > 详情

认领

导出

Link by DOI

反馈

作者信息关键词期刊信息基础信息归属信息摘要

成果类型：

期刊论文

作者：

She, Wenyan;Liu, Tingting;Li, Haimei;Wang, Zichen;Guo, Zhibin;...

通讯作者：

Liu, Y;Liu, Yi;Liu, YJ

作者机构：

[She, Wenyan; Wang, Zichen; Liu, Yi; Liu, Yujiao; Li, Haimei] Wuhan Univ, Coll Chem & Mol Sci, Wuhan 430072, Peoples R China.

[Liu, Yujiao; Liu, Tingting; Guo, Zhibin; Liu, Yi; Liu, YJ] Tiangong Univ, State Key Lab Separat Membranes & Membrane Proc, Sch Chem, Tianjin 300387, Peoples R China.

[Liu, Yujiao; Liu, Tingting; Guo, Zhibin; Liu, Yi; Liu, YJ] Tiangong Univ, Sch Mat Sci & Engn, Tianjin 300387, Peoples R China.

[Liu, Yi; Liu, Yujiao] Wuhan Polytech Univ, Sch Chem & Environm Engn, Wuhan 430023, Peoples R China.

[Liu, Yi; Liu, Yujiao] Hubei Univ Sci & Technol, Hubei Key Lab Radiat Chem & Funct Mat, Xianning 437100, Peoples R China.

通讯机构：

[Liu, Y; Liu, YJ ] T

[Liu, Y ] W

Wuhan Univ, Coll Chem & Mol Sci, Wuhan 430072, Peoples R China.

Tiangong Univ, State Key Lab Separat Membranes & Membrane Proc, Sch Chem, Tianjin 300387, Peoples R China.

Tiangong Univ, Sch Mat Sci & Engn, Tianjin 300387, Peoples R China.

语种：

英文

期刊：

JOURNAL OF MEDICINAL CHEMISTRY

ISSN：

0022-2623

年：

2023

卷：

期：

页码：

14683-14699

DOI：

10.1021/acs.jmedchem.3c01197

基金类别：

National Natural Science Foundation of China [22073070]; Science and Technology Plans of Tianjin [22ZYIDSS00070]

机构署名：

本校为通讯机构

院系归属：

化学与环境工程学院

摘要：

In many types of cancers, pyruvate dehydrogenase kinase (PDK) is abnormally overexpressed and has become a promising target for cancer therapy. However, few highly effective inhibitors of PDK have been reported to date. Herein, we designed and synthesized a series of PDK inhibitors based on dichloroacetate (DCA) and arsenicals. Of the 27 compounds, 1f demonstrated PDK inhibition with high efficiency at a cellular level (IC(50) = 2.0 μM) and an enzyme level (EC(50) = 68 nM), far more effective than that of DCA. In silico, in vitro, and in vivo ...

反馈

产权有误：本人成果被他人认领

数据有误：数据基本信息有误

归属有误：成果的院系归属、机构署名归属有误

其他原因：

验证码：

看不清楚，换一个

确定

取消

成果认领

标题：

用户	作者	通讯作者	--
	请选择	请选择	--

确定

取消

Reprogramming Energy Metabolism with Synthesized PDK Inhibitors Based on Dichloroacetate Derivatives and Targeted Delivery Systems for Enhanced Cancer Therapy

反馈

成果认领

提示

该栏目需要登录且有访问权限才可以访问