Inhibition of WAC alleviates the chondrocyte proinflammatory secretory phenotype and cartilage degradation via H2BK120ub1 and H3K27me3 coregulation

Several types of arthritis share the common feature that the generation of inflammatory mediators leads to joint cartilage degradation. However, the shared mechanism is largely unknown. H2BK120ub1 was reportedly involved in various inflammatory diseases but its role in the shared mechanism in inflam...

Full description

Saved in:
Bibliographic Details
Main Authors: Peitao Xu, Guiwen Ye, Xiaojun Xu, Zhidong Liu, Wenhui Yu, Guan Zheng, Zepeng Su, Jiajie Lin, Yunshu Che, Yipeng Zeng, Zhikun Li, Pei Feng, Qian Cao, Zhongyu Xie, Yanfeng Wu, Huiyong Shen, Jinteng Li
Format: Article
Language:English
Published: Elsevier 2025-08-01
Series:Acta Pharmaceutica Sinica B
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S2211383525004356
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1849233533022765056
author Peitao Xu
Guiwen Ye
Xiaojun Xu
Zhidong Liu
Wenhui Yu
Guan Zheng
Zepeng Su
Jiajie Lin
Yunshu Che
Yipeng Zeng
Zhikun Li
Pei Feng
Qian Cao
Zhongyu Xie
Yanfeng Wu
Huiyong Shen
Jinteng Li
author_facet Peitao Xu
Guiwen Ye
Xiaojun Xu
Zhidong Liu
Wenhui Yu
Guan Zheng
Zepeng Su
Jiajie Lin
Yunshu Che
Yipeng Zeng
Zhikun Li
Pei Feng
Qian Cao
Zhongyu Xie
Yanfeng Wu
Huiyong Shen
Jinteng Li
author_sort Peitao Xu
collection DOAJ
description Several types of arthritis share the common feature that the generation of inflammatory mediators leads to joint cartilage degradation. However, the shared mechanism is largely unknown. H2BK120ub1 was reportedly involved in various inflammatory diseases but its role in the shared mechanism in inflammatory joint conditions remains elusive. The present study demonstrated that levels of cartilage degradation, H2BK120ub1, and its regulator WW domain-containing adapter protein with coiled-coil (WAC) were increased in cartilage in human rheumatoid arthritis (RA) and osteoarthritis (OA) patients as well as in experimental RA and OA mice. By regulating H2BK120ub1 and H3K27me3, WAC regulated the secretion of inflammatory and cartilage-degrading factors. WAC influenced the level of H3K27me3 by regulating nuclear entry of the H3K27 demethylase KDM6B, and acted as a key factor of the crosstalk between H2BK120ub1 and H3K27me3. The cartilage-specific knockout of WAC demonstrated the ability to alleviate cartilage degradation in collagen-induced arthritis (CIA) and collagenase-induced osteoarthritis (CIOA) mice. Through molecular docking and dynamic simulation, doxercalciferol was found to inhibit WAC and the development of cartilage degradation in the CIA and CIOA models. Our study demonstrated that WAC is a key factor of cartilage degradation in arthritis, and targeting WAC by doxercalciferol could be a viable therapeutic strategy for treating cartilage destruction in several types of arthritis.
format Article
id doaj-art-33ecd5a29a024ed0818137617f2ff024
institution Kabale University
issn 2211-3835
language English
publishDate 2025-08-01
publisher Elsevier
record_format Article
series Acta Pharmaceutica Sinica B
spelling doaj-art-33ecd5a29a024ed0818137617f2ff0242025-08-20T05:06:38ZengElsevierActa Pharmaceutica Sinica B2211-38352025-08-011584064407710.1016/j.apsb.2025.06.015Inhibition of WAC alleviates the chondrocyte proinflammatory secretory phenotype and cartilage degradation via H2BK120ub1 and H3K27me3 coregulationPeitao Xu0Guiwen Ye1Xiaojun Xu2Zhidong Liu3Wenhui Yu4Guan Zheng5Zepeng Su6Jiajie Lin7Yunshu Che8Yipeng Zeng9Zhikun Li10Pei Feng11Qian Cao12Zhongyu Xie13Yanfeng Wu14Huiyong Shen15Jinteng Li16Department of Orthopedics, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, ChinaDepartment of Orthopedics, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, ChinaDepartment of Orthopedics, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, ChinaDepartment of Orthopedics, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, ChinaDepartment of Orthopedics, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, ChinaDepartment of Orthopedics, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, ChinaDepartment of Orthopedics, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, ChinaDepartment of Orthopedics, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, ChinaDepartment of Orthopedics, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, ChinaDepartment of Orthopedics, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, ChinaDepartment of Orthopedics, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, ChinaCenter for Biotherapy, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, ChinaCenter for Biotherapy, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, ChinaDepartment of Orthopedics, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, ChinaCenter for Biotherapy, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, China; Corresponding authors.Department of Orthopedics, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, China; Corresponding authors.Department of Orthopedics, the Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen 518003, China; Corresponding authors.Several types of arthritis share the common feature that the generation of inflammatory mediators leads to joint cartilage degradation. However, the shared mechanism is largely unknown. H2BK120ub1 was reportedly involved in various inflammatory diseases but its role in the shared mechanism in inflammatory joint conditions remains elusive. The present study demonstrated that levels of cartilage degradation, H2BK120ub1, and its regulator WW domain-containing adapter protein with coiled-coil (WAC) were increased in cartilage in human rheumatoid arthritis (RA) and osteoarthritis (OA) patients as well as in experimental RA and OA mice. By regulating H2BK120ub1 and H3K27me3, WAC regulated the secretion of inflammatory and cartilage-degrading factors. WAC influenced the level of H3K27me3 by regulating nuclear entry of the H3K27 demethylase KDM6B, and acted as a key factor of the crosstalk between H2BK120ub1 and H3K27me3. The cartilage-specific knockout of WAC demonstrated the ability to alleviate cartilage degradation in collagen-induced arthritis (CIA) and collagenase-induced osteoarthritis (CIOA) mice. Through molecular docking and dynamic simulation, doxercalciferol was found to inhibit WAC and the development of cartilage degradation in the CIA and CIOA models. Our study demonstrated that WAC is a key factor of cartilage degradation in arthritis, and targeting WAC by doxercalciferol could be a viable therapeutic strategy for treating cartilage destruction in several types of arthritis.http://www.sciencedirect.com/science/article/pii/S2211383525004356ArthritisWACCartilage degradationChondrocyte secretionHistone modificationDoxercalciferol
spellingShingle Peitao Xu
Guiwen Ye
Xiaojun Xu
Zhidong Liu
Wenhui Yu
Guan Zheng
Zepeng Su
Jiajie Lin
Yunshu Che
Yipeng Zeng
Zhikun Li
Pei Feng
Qian Cao
Zhongyu Xie
Yanfeng Wu
Huiyong Shen
Jinteng Li
Inhibition of WAC alleviates the chondrocyte proinflammatory secretory phenotype and cartilage degradation via H2BK120ub1 and H3K27me3 coregulation
Acta Pharmaceutica Sinica B
Arthritis
WAC
Cartilage degradation
Chondrocyte secretion
Histone modification
Doxercalciferol
title Inhibition of WAC alleviates the chondrocyte proinflammatory secretory phenotype and cartilage degradation via H2BK120ub1 and H3K27me3 coregulation
title_full Inhibition of WAC alleviates the chondrocyte proinflammatory secretory phenotype and cartilage degradation via H2BK120ub1 and H3K27me3 coregulation
title_fullStr Inhibition of WAC alleviates the chondrocyte proinflammatory secretory phenotype and cartilage degradation via H2BK120ub1 and H3K27me3 coregulation
title_full_unstemmed Inhibition of WAC alleviates the chondrocyte proinflammatory secretory phenotype and cartilage degradation via H2BK120ub1 and H3K27me3 coregulation
title_short Inhibition of WAC alleviates the chondrocyte proinflammatory secretory phenotype and cartilage degradation via H2BK120ub1 and H3K27me3 coregulation
title_sort inhibition of wac alleviates the chondrocyte proinflammatory secretory phenotype and cartilage degradation via h2bk120ub1 and h3k27me3 coregulation
topic Arthritis
WAC
Cartilage degradation
Chondrocyte secretion
Histone modification
Doxercalciferol
url http://www.sciencedirect.com/science/article/pii/S2211383525004356
work_keys_str_mv AT peitaoxu inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT guiwenye inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT xiaojunxu inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT zhidongliu inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT wenhuiyu inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT guanzheng inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT zepengsu inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT jiajielin inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT yunshuche inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT yipengzeng inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT zhikunli inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT peifeng inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT qiancao inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT zhongyuxie inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT yanfengwu inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT huiyongshen inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation
AT jintengli inhibitionofwacalleviatesthechondrocyteproinflammatorysecretoryphenotypeandcartilagedegradationviah2bk120ub1andh3k27me3coregulation