Small-molecule inhibition of TLR8 through stabilization of its resting state

Shuting Zhang,Zhenyi Hu,Hiromi Tanji,Shuangshuang Jiang,Nabanita Das,Jing Li,Kentaro Sakaniwa,Jin Jin, Yanyan Bian,Umeharu Ohto,Toshiyuki Shimizu,Hang Yin

NATURE CHEMICAL BIOLOGY（2017）

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摘要

High-throughput screening identified potent small-molecule inhibitors of the endosomal Toll-like receptor TLR8 that stabilize the preformed TLR8 dimer in its resting state by binding to a unique site on the inactive dimer interface.

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关键词

Mechanism of action,Small molecules,X-ray crystallography,Chemistry/Food Science,general,Biochemical Engineering,Biochemistry,Cell Biology,Bioorganic Chemistry

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