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靶向先天免疫受体 TLR8 的小分子药物。

Targeting the innate immune receptor TLR8 using small-molecule agents.

机构信息

Graduate School of Pharmaceutical Sciences, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.

出版信息

Acta Crystallogr D Struct Biol. 2020 Jul 1;76(Pt 7):621-629. doi: 10.1107/S2059798320006518. Epub 2020 Jun 17.

DOI:10.1107/S2059798320006518
PMID:32627735
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7336380/
Abstract

Toll-like receptors (TLRs) are pattern-recognition receptors that initiate innate immune responses. Among the TLRs, TLR8 (and TLR7) recognizes single-stranded RNA to mediate downstream signals. In recent years, intensive X-ray crystal structural analyses have provided atomic insights into structures of TLR8 complexed with various agonists or antagonists. Here, structural knowledge of the activation and inactivation mechanisms of the ligands is reviewed. In addition, the potential clinical applications of TLR ligands are examined.

摘要

Toll 样受体（TLRs）是一种模式识别受体，可启动先天免疫反应。在 TLRs 中，TLR8（和 TLR7）识别单链 RNA 以介导下游信号。近年来，密集的 X 射线晶体结构分析为 TLR8 与各种激动剂或拮抗剂复合物的结构提供了原子水平的见解。本文综述了配体激活和失活机制的结构知识。此外，还研究了 TLR 配体的潜在临床应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e5a/7336380/2e8c04e7f99e/d-76-00621-fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e5a/7336380/dd4800311c7f/d-76-00621-fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e5a/7336380/88906949089e/d-76-00621-fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e5a/7336380/84fe18f1fb9e/d-76-00621-fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e5a/7336380/cb08939a9be8/d-76-00621-fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e5a/7336380/51bf2815dfec/d-76-00621-fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e5a/7336380/2e8c04e7f99e/d-76-00621-fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e5a/7336380/dd4800311c7f/d-76-00621-fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e5a/7336380/88906949089e/d-76-00621-fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e5a/7336380/84fe18f1fb9e/d-76-00621-fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e5a/7336380/cb08939a9be8/d-76-00621-fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e5a/7336380/51bf2815dfec/d-76-00621-fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e5a/7336380/2e8c04e7f99e/d-76-00621-fig6.jpg

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