Cartilage targeting hydrogel nanoplatform degrades BRD4 to alleviate osteoarthritis via Nav1.7 axis

Osteoarthritis (OA) is a common degenerative joint disease with limited disease-modifying therapies. Emerging evidence suggests that epigenetic dysregulation contributes to cartilage degeneration, but effective strategies to selectively target these pathways remain lacking. Here we show that the BRD4/Nav1.7 axis drives inflammatory and metabolic dysfunction in OA. Integrated single-cell and transcriptomic analyses identify BRD4 as a key regulator that enhances Nav1.7 transcription, promoting mitochondrial impairment and catabolic activation in chondrocytes. To therapeutically target this pathway, we develop a biomimetic hydrogel system incorporating chondrocyte membrane-coated nanoparticles for cartilage-specific delivery of a BRD4 proteolysis-targeting chimera (PROTAC), a molecule designed to induce selective protein degradation. This nanoplatform enables efficient intra-articular delivery, immune evasion and targeted retention in cartilage. Treatment suppresses inflammatory responses, restores mitochondrial function and reduces cartilage degeneration and pain behaviors in two mouse models of OA. These findings establish targeted BRD4 degradation as a disease-modifying strategy and provide a precision nanotherapeutic platform for OA.

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Publication Details

Journal
Nature Communications
Published
2026-03-28
DOI
https://doi.org/10.1038/s41467-026-71246-w
Primary Topic
Protein Degradation and Inhibitors
Type
article
Field-Weighted Citation Impact
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article

Cartilage targeting hydrogel nanoplatform degrades BRD4 to alleviate osteoarthritis via Nav1.7 axis

Zixuan Gao, D. X. Cui, Qiang Lou, Bo Zhu et al.
Nature Communications
Protein Degradation and Inhibitors
article

Cartilage targeting hydrogel nanoplatform degrades BRD4 to alleviate osteoarthritis via Nav1.7 axis

Zixuan Gao, D. X. Cui, Qiang Lou, Bo Zhu, Qirui Zhao, Wei Wang, Yanlei Liu, Tongtong Xu, Z H Liu, X P Lu, Zhiming Song, Zhe Yu, Jesus M M. de la Fuente, Jiaming Li, Hui Zhao, Yan Zhang, Hui Liang, Guangjie Yang, Zuchao Du, Zhiguang Ren, Linjia Peng
article en

Abstract

Osteoarthritis (OA) is a common degenerative joint disease with limited disease-modifying therapies. Emerging evidence suggests that epigenetic dysregulation contributes to cartilage degeneration, but effective strategies to selectively target these pathways remain lacking. Here we show that the BRD4/Nav1.7 axis drives inflammatory and metabolic dysfunction in OA. Integrated single-cell and transcriptomic analyses identify BRD4 as a key regulator that enhances Nav1.7 transcription, promoting mitochondrial impairment and catabolic activation in chondrocytes. To therapeutically target this pathway, we develop a biomimetic hydrogel system incorporating chondrocyte membrane-coated nanoparticles for cartilage-specific delivery of a BRD4 proteolysis-targeting chimera (PROTAC), a molecule designed to induce selective protein degradation. This nanoplatform enables efficient intra-articular delivery, immune evasion and targeted retention in cartilage. Treatment suppresses inflammatory responses, restores mitochondrial function and reduces cartilage degeneration and pain behaviors in two mouse models of OA. These findings establish targeted BRD4 degradation as a disease-modifying strategy and provide a precision nanotherapeutic platform for OA.

Nature Communications
Henan University (CN), Shanghai Jiao Tong University (CN), Instituto de Nanociencia y Materiales de Aragón (ES), First Affiliated Hospital of Henan University (CN)
Good health and well-being
Openalex Percentile: Top 5%
Protein Degradation and Inhibitors
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