Nature Communications (Oct 2020)
Structural analysis reveals TLR7 dynamics underlying antagonism
- Shingo Tojo,
- Zhikuan Zhang,
- Hiroyuki Matsui,
- Masahiro Tahara,
- Mitsunori Ikeguchi,
- Mami Kochi,
- Mami Kamada,
- Hideki Shigematsu,
- Akihisa Tsutsumi,
- Naruhiko Adachi,
- Takuma Shibata,
- Masaki Yamamoto,
- Masahide Kikkawa,
- Toshiya Senda,
- Yoshiaki Isobe,
- Umeharu Ohto,
- Toshiyuki Shimizu
Affiliations
- Shingo Tojo
- Sumitomo Dainippon Pharma Co., Ltd.
- Zhikuan Zhang
- Graduate School of Pharmaceutical Sciences, The University of Tokyo
- Hiroyuki Matsui
- Sumitomo Dainippon Pharma Co., Ltd.
- Masahiro Tahara
- Sumitomo Dainippon Pharma Co., Ltd.
- Mitsunori Ikeguchi
- Graduate School of Medical Life Science, Yokohama City University
- Mami Kochi
- Sumitomo Dainippon Pharma Co., Ltd.
- Mami Kamada
- Sumitomo Dainippon Pharma Co., Ltd.
- Hideki Shigematsu
- RIKEN SPring-8 Center
- Akihisa Tsutsumi
- Department of Cell Biology and Anatomy, Graduate School of Medicine, the University of Tokyo
- Naruhiko Adachi
- Structural Biology Research Center, Institute of Materials Structure Science, High Energy Accelerator Research Organization (KEK)
- Takuma Shibata
- Division of Innate Immunity, Department of Microbiology and Immunology, The Institute of Medical Science, The University of Tokyo
- Masaki Yamamoto
- RIKEN SPring-8 Center
- Masahide Kikkawa
- Department of Cell Biology and Anatomy, Graduate School of Medicine, the University of Tokyo
- Toshiya Senda
- Structural Biology Research Center, Institute of Materials Structure Science, High Energy Accelerator Research Organization (KEK)
- Yoshiaki Isobe
- Sumitomo Dainippon Pharma Co., Ltd.
- Umeharu Ohto
- Graduate School of Pharmaceutical Sciences, The University of Tokyo
- Toshiyuki Shimizu
- Graduate School of Pharmaceutical Sciences, The University of Tokyo
- DOI
- https://doi.org/10.1038/s41467-020-19025-z
- Journal volume & issue
-
Vol. 11,
no. 1
pp. 1 – 11
Abstract
A series of Toll-like receptor 7 (TLR7)-specific antagonists and extensive structural analysis reveal the open conformation of the receptor and the structural basis of TLR7 antagonism. One of the compounds shows efficacy in treating mouse model of systemic lupus erythematosus.