Cited by 476Immune Response and InflammationReceptor Mechanisms and SignalingInflammasome and immune disorders

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Structural Analysis Reveals that Toll-like Receptor 7 Is a Dual Receptor for Guanosine and Single-Stranded RNA

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Zhang, Zhikuan, Ohto, Umeharu, Shibata, Takuma, Krayukhina, Elena, Taoka, Masato, Yamauchi, Yoshio, Tanji, Hiromi, Isobe, Toshiaki, Uchiyama, Susumu, Miyake, Kensuke, Shimizu, Toshiyuki·2016·Immunity

DOI 10.1016/j.immuni.2016.09.011

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Abstract

Toll-like receptor 7 (TLR7) is a single-stranded RNA (ssRNA) sensor in innate immunity and also responds to guanosine and chemical ligands, such as imidazoquinoline compounds. However, TLR7 activation mechanism by these ligands remain largely unknown. Here, we generated crystal structures of three TLR7 complexes, and found that all formed an activated m-shaped dimer with two ligand-binding sites. The first site conserved in TLR7 and TLR8 was used for small ligand-binding essential for its activation. The second site spatially distinct from that of TLR8 was used for a ssRNA-binding that enhanced the affinity of the first-site ligands. The first site preferentially recognized guanosine and the second site specifically bound to uridine moieties in ssRNA. Our structural, biochemical, and mutagenesis studies indicated that TLR7 is a dual receptor for guanosine and uridine-containing ssRNA. Our findings have important implications for understanding of TLR7 function, as well as for therapeutic manipulation of TLR7 activation.

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Additional file 8 of MicroRNA-100-5p and microRNA-298-5p released from apoptotic cortical neurons are endogenous Toll-like receptor 7/8 ligands that contribute to neurodegeneration
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Authors: Zhang, Z., Ohto, U., Shibata, T., Krayukhina, E., Taoka, M., Yamauchi, Y., Tanji, H., Isobe, T., Uchiyama, S., Miyake, K., & Shimizu, T.
Affiliations: The University of Tokyo (JP)
Institute of Medical Science, The University of Tokyo (JP)
The University of Osaka (JP)
Tokyo Metropolitan University (JP)
National Institutes of Natural Sciences (JP)
Corresponding author: Shimizu, Toshiyuki
ORCID: Ohto, Umeharu
Shibata, Takuma
Taoka, Masato
Yamauchi, Yoshio
Isobe, Toshiaki
Uchiyama, Susumu
Miyake, Kensuke
Shimizu, Toshiyuki
Venue: Immunity
Publisher: Elsevier BV
Published: 2016-10
Volume: 45
Issue: 4
Pages: 737-748
ISSN: 1074-7613 (ISSN-L)
DOI: 10.1016/j.immuni.2016.09.011
OpenAlex: W2530273804
Cited by: 461
References: 48
Citations by year: 2026: 34 · 2025: 45 · 2024: 57 · 2023: 56 · 2022: 46 · 2021: 66 · 2020: 44 · 2019: 41 · 2018: 43 · 2017: 25 · 2016: 4
FWCI: 23.05
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
www.elsevier.com/open-access/userlicense/1.0/ (vor, 382 d)
doi.org/10.15223/policy-017 (stm-asf)
doi.org/10.15223/policy-037 (stm-asf)
doi.org/10.15223/policy-012 (stm-asf)
doi.org/10.15223/policy-029 (stm-asf)
doi.org/10.15223/policy-004 (stm-asf)
Locations: Immunity (publishedVersion)
PubMed (publishedVersion)
Funders: Daiichi Sankyo Foundation of Life Science
Ministry of Education, Culture, Sports, Science and Technology
Mochida Memorial Foundation for Medical and Pharmaceutical Research
Topics: Life Sciences › Immunology and Microbiology › Immunology › Immune Response and Inflammation
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Inflammasome and immune disorders
Keywords: TLR7, guanosine, single-stranded RNA, uridine, imidazoquinolines, ligand binding sites, receptor dimerization, innate immunity, crystal structure, TLR8
MeSH terms: Animals, Binding Sites, Cell Line, Drosophila, Guanosine, Humans, Immunity, Innate, Ligands, Macaca mulatta, RNA, Toll-Like Receptor 7, HEK293 Cells

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Structural Analysis Reveals that Toll-like Receptor 7 Is a Dual Receptor for Guanosine and Single-Stranded RNA

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