%0 Journal Article
%T A chemical approach for global protein knockdown from mice to non-human primates
%A Guangju Ji
%A Jianguo Zhao
%A Jun Wang
%A Liguo Wang
%A Qiuye Zhao
%A Rui-Ping Xiao
%A Tianlong Lan
%A Wen Zheng
%A Xia Yao
%A Xinyi Zhang
%A Xiuqin Zhang
%A Xiuyun Sun
%A Yang Mao
%A Yonghui Sun
%A Yu Rao
%J Archive of "Cell Discovery".
%D 2019
%R 10.1038/s41421-018-0079-1
%X a Mechanism of action of PROTAC. b Docking mode of RC32 binding to FKBP12 and recruiting CRBN. Moiety in red, linker; moiety in blue, rapamycin; moiety in green, pomalimide. c Chemical structure of RC32. d Immunoblots showing degradation of FKBP12 in Jurkat cells treated with RC32 at the indicated concentrations for 12£¿h. £¿-Actin served as a loading control. e Immunoblots for FKBP12 protein. Jurkat cells were first treated for 3£¿h with bortezomib (Bortez), carfilzomib (Carf), rapamycin (RAP), or pomalimide (Poma) followed by treatment with RC32 (10£¿nM) for 2£¿h. £¿-Actin served as a loading control. f DC50 with 12£¿h of RC32 treatment in Jurkat cells. g Recovery of FKBP12 level after washout of RC32. After treatment for 12£¿h with 1£¿¦ÌM RC32, the Jurkat cells were washed with fresh culture medium and further cultured in fresh medium for the indicated times. h Selectivity of RC32 against FKBPs in Jurkat cells. i Degradation efficiency of RC32 in different cell lines (100£¿nM) and primary cardiac myocytes (1£¿¦ÌM) treated for 12£¿h. Data in (f) and (i) are presented as mean£¿¡À£¿SEM of 3 independent experiment
%U https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6361926/