Trimannose-coupled antimiR-21 for macrophage-targeted inhalation treatment of acute inflammatory lung damage.


Journal

Nature communications
ISSN: 2041-1723
Titre abrégé: Nat Commun
Pays: England
ID NLM: 101528555

Informations de publication

Date de publication:
28 07 2023
Historique:
received: 23 12 2022
accepted: 18 07 2023
medline: 31 7 2023
pubmed: 29 7 2023
entrez: 28 7 2023
Statut: epublish

Résumé

Recent studies of severe acute inflammatory lung disease including COVID-19 identify macrophages to drive pulmonary hyperinflammation and long-term damage such as fibrosis. Here, we report on the development of a first-in-class, carbohydrate-coupled inhibitor of microRNA-21 (RCS-21), as a therapeutic means against pulmonary hyperinflammation and fibrosis. MicroRNA-21 is among the strongest upregulated microRNAs in human COVID-19 and in mice with acute inflammatory lung damage, and it is the strongest expressed microRNA in pulmonary macrophages. Chemical linkage of a microRNA-21 inhibitor to trimannose achieves rapid and specific delivery to macrophages upon inhalation in mice. RCS-21 reverses pathological activation of macrophages and prevents pulmonary dysfunction and fibrosis after acute lung damage in mice. In human lung tissue infected with SARS-CoV-2 ex vivo, RCS-21 effectively prevents the exaggerated inflammatory response. Our data imply trimannose-coupling for effective and selective delivery of inhaled oligonucleotides to pulmonary macrophages and report on a first mannose-coupled candidate therapeutic for COVID-19.

Identifiants

pubmed: 37507393
doi: 10.1038/s41467-023-40185-1
pii: 10.1038/s41467-023-40185-1
pmc: PMC10382532
doi:

Substances chimiques

MicroRNAs 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

4564

Informations de copyright

© 2023. The Author(s).

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Auteurs

Christina Beck (C)

Institute of Pharmacology and Toxicology, Technical University of Munich (TUM), Munich, Germany.
DZHK (German Centre for Cardiovascular Research), partner site Munich Heart Alliance, Munich, Germany.

Deepak Ramanujam (D)

Institute of Pharmacology and Toxicology, Technical University of Munich (TUM), Munich, Germany.
DZHK (German Centre for Cardiovascular Research), partner site Munich Heart Alliance, Munich, Germany.
RNATICS GmbH, Planegg-Martinsried, Germany.

Paula Vaccarello (P)

Institute of Pharmacology and Toxicology, Technical University of Munich (TUM), Munich, Germany.

Florenc Widenmeyer (F)

Institute of Pharmacology and Toxicology, Technical University of Munich (TUM), Munich, Germany.

Martin Feuerherd (M)

Institute of Virology, Helmholtz Munich, Technical University of Munich (TUM), School of Medicine, Munich, Germany.

Cho-Chin Cheng (CC)

Institute of Virology, Helmholtz Munich, Technical University of Munich (TUM), School of Medicine, Munich, Germany.

Anton Bomhard (A)

Institute of Pharmacology and Toxicology, Technical University of Munich (TUM), Munich, Germany.

Tatiana Abikeeva (T)

Institute of Pharmacology and Toxicology, Technical University of Munich (TUM), Munich, Germany.

Julia Schädler (J)

Institute of Legal Medicine, University Medical Center Hamburg-Eppendorf, Hamburg, Germany.

Jan-Peter Sperhake (JP)

Institute of Legal Medicine, University Medical Center Hamburg-Eppendorf, Hamburg, Germany.

Matthias Graw (M)

Institute of Legal Medicine, Faculty of Medicine, Ludwig-Maximilians-Universität (LMU) München, Munich, Germany.

Seyer Safi (S)

Division of Thoracic Surgery, Klinikum rechts der Isar, Technical University of Munich (TUM), Munich, Germany.

Hans Hoffmann (H)

Division of Thoracic Surgery, Klinikum rechts der Isar, Technical University of Munich (TUM), Munich, Germany.

Claudia A Staab-Weijnitz (CA)

Comprehensive Pneumology Center, Institute of Lung Health and Immunity, Helmholtz Center Munich, Member of the German Center of Lung Research (DZL), Munich, Germany.

Roland Rad (R)

Institute of Molecular Oncology and Functional Genomics, Translatum Cancer Center, School of Medicine, Technical University of Munich (TUM), Munich, Germany.

Ulrike Protzer (U)

Institute of Virology, Helmholtz Munich, Technical University of Munich (TUM), School of Medicine, Munich, Germany.
German Center for Infection Research (DZIF), partner site Munich, Munich, Germany.

Thomas Frischmuth (T)

Baseclick GmbH, Neuried, Germany.
RNATICS GmbH, Planegg-Martinsried, Germany.

Stefan Engelhardt (S)

Institute of Pharmacology and Toxicology, Technical University of Munich (TUM), Munich, Germany. Stefan.engelhardt@tum.de.
DZHK (German Centre for Cardiovascular Research), partner site Munich Heart Alliance, Munich, Germany. Stefan.engelhardt@tum.de.

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