维普期刊资源整合服务平台（V6.5）

维普中文期刊产品整合服务

1篇 您的检索式：作者名="Christopher L.Antos"

选中清除导出查看参考文献查看引证文献引用追踪共1页首页上一页第1页下一页末页 /1 跳转

		题名	作者	年代	出处	被引量
	1	Discovery of a subtype-selective, covalent inhibitor against palmitoylation pocket of TEAD3显示文摘The TEA domain(TEAD)family proteins(TEAD1-4)are essential transcription factors that control cell differentiation and organ size in the Hippo pathway.Although the sequences and structures of TEAD family proteins are highly conserved,each TEAD isoform has unique physiological and pathological functions.Therefore,the development and discovery of subtype selective inhibitors for TEAD protein will provide important chemical probes for the TEAD-related function studies in development and diseases.Here,we identified a novel TEAD 1/3 covalent inhibitor(DC-TEADin1072)with biochemical IC50 values of 0.61±0.02 and 0.58±0.12μmol/L against TEAD1 and TEAD3,respectively.Further chemical optimization based on DC-TEAD in 1072 yielded a selective TEAD3 inhibitor DCTEAD3 in03 with the IC_(50) value of 0.16±0.03μmol/L,which shows 100-fold selectivity over other TEAD isoforms in activity-based protein profiling(ABPP)assays.In cells,DC-TEAD3 in03 showed selective inhibitory effect on TEAD3 in GAL4-TEAD(1-4)reporter assays with the IC50 value of1.15μmol/L.When administered to zebrafish juveniles,experiments showed that DC-TEAD3 in03 reduced the growth rate of zebrafish caudal fins,indicating the importance of TEAD3 activity in controlling proportional growth of vertebrate appendages.	Tian Lu Yong Li Wenchao Lu TWGM Spitters Xueyu Fang Jun Wang Simian Cai Jing Gao Yanting Zhou Zhe Duan Huan Xiong Liping Liu Qi Li Hualiang Jiang Kaixian Chen Hu Zhou Hua Lin Huijin Feng Bing Zhou Christopher L.Antos Cheng Luo	2021	Acta Pharmaceutica Sinica B2021，11，10：	0

返回顶部每页显示：

共1页首页上一页第1页下一页末页 /1 跳转

goolge学术搜索-维普

网站首页 | 关于我们 | 联系我们 | 产品服务 | 客服中心 | 广告服务 | 版权声明 | 网站联盟 | 友情链接 | 售卡网点

版权所有© 渝B2-20050021-1　渝公网安备 50019002500403号　违法和不良信息举报中心

互联网出版许可证新出网证(渝)字10号全国400电话 - 免长途话费