Inhibition of ARH2 by pH/ROS-responsive nanosystem for improved lung adenocarcinoma immunochemotherapy

Immunotherapy resistance remains a substantial barrier to improving treatment outcomes for patients with lung adenocarcinoma (LUAD). Identifying effective immunotherapy target is crucial for enhancing therapeutic efficacy in LUAD. Through database analysis, we discovered that ADP ribosylhydrolase-li...

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Main Authors: Rui Cai, Meng Wang, Mengting Pan, Zhiwu Zhang, Qiang Jia, Longbao Feng, Zhongjian Yu, Lu Liu, Tongyu Zhu, Silin Cai, Han Tian, Jiangyu Zhang, Rui Guo, Yanfang Zheng
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Language:English
Published: KeAi Communications Co., Ltd. 2025-11-01
Series:Bioactive Materials
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Online Access:http://www.sciencedirect.com/science/article/pii/S2452199X25003354
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author Rui Cai
Meng Wang
Mengting Pan
Zhiwu Zhang
Qiang Jia
Longbao Feng
Zhongjian Yu
Lu Liu
Tongyu Zhu
Silin Cai
Han Tian
Jiangyu Zhang
Rui Guo
Yanfang Zheng
author_facet Rui Cai
Meng Wang
Mengting Pan
Zhiwu Zhang
Qiang Jia
Longbao Feng
Zhongjian Yu
Lu Liu
Tongyu Zhu
Silin Cai
Han Tian
Jiangyu Zhang
Rui Guo
Yanfang Zheng
author_sort Rui Cai
collection DOAJ
description Immunotherapy resistance remains a substantial barrier to improving treatment outcomes for patients with lung adenocarcinoma (LUAD). Identifying effective immunotherapy target is crucial for enhancing therapeutic efficacy in LUAD. Through database analysis, we discovered that ADP ribosylhydrolase-like 1 (ADPRHL1, ARH2) is associated with immunosuppression. In this study, we first demonstrated that the increased presence of ARH2-positive macrophages in LUAD tumors is associated with immunosuppression. Furthermore, ARH2 promotes M2 macrophage polarization and suppresses immune responses by regulating the FPR2/PI3K/AKT signaling pathway. Additionally, we found that artesunate (ART) can induce necroptosis in LUAD cells and activate antitumor immune responses. To translate these findings into a clinically viable therapeutic approach, we developed a pH/ROS-responsive nanosystem capable of co-delivering siARH2 and ART. This nanosystem effectively activated immune responses in both tumor cells and tumor-associated macrophages. Furthermore, the nanosystem demonstrated excellent in vivo safety, precise PD-L1 targeting, and responsiveness to ROS and pH variations. It considerably suppressed the malignant phenotype of tumor cells induced by macrophages and enhanced T-cell-mediated immune responses. Overall, targeting ARH2 in combination with ART represents a promising novel strategy for the treatment of LUAD.
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spelling doaj-art-93be76bf9b1940e6aa6f6ee150b58d892025-08-20T03:41:58ZengKeAi Communications Co., Ltd.Bioactive Materials2452-199X2025-11-015373775310.1016/j.bioactmat.2025.07.042Inhibition of ARH2 by pH/ROS-responsive nanosystem for improved lung adenocarcinoma immunochemotherapyRui Cai0Meng Wang1Mengting Pan2Zhiwu Zhang3Qiang Jia4Longbao Feng5Zhongjian Yu6Lu Liu7Tongyu Zhu8Silin Cai9Han Tian10Jiangyu Zhang11Rui Guo12Yanfang Zheng13Guangzhou Institute of Cancer Research, The Affiliated Cancer Hospital, Guangzhou Medical University, Guangzhou, 510095, China; State Key Laboratory of Respiratory Disease, Guangzhou, 510180, ChinaGuangzhou Institute of Cancer Research, The Affiliated Cancer Hospital, Guangzhou Medical University, Guangzhou, 510095, China; State Key Laboratory of Respiratory Disease, Guangzhou, 510180, ChinaGuangzhou Institute of Cancer Research, The Affiliated Cancer Hospital, Guangzhou Medical University, Guangzhou, 510095, China; State Key Laboratory of Respiratory Disease, Guangzhou, 510180, ChinaGuangzhou Institute of Cancer Research, The Affiliated Cancer Hospital, Guangzhou Medical University, Guangzhou, 510095, China; State Key Laboratory of Respiratory Disease, Guangzhou, 510180, ChinaGuangzhou City Polytechnic, Guangzhou, 510405, ChinaKey Laboratory of Biomaterials of Guangdong Higher Education Institutes, Guangdong Provincial Engineering and Technological Research Center for Drug Carrier Development, Department of Biomedical Engineering, Jinan University, Guangzhou, 510632, ChinaGuangzhou Institute of Cancer Research, The Affiliated Cancer Hospital, Guangzhou Medical University, Guangzhou, 510095, China; State Key Laboratory of Respiratory Disease, Guangzhou, 510180, ChinaGuangzhou Institute of Cancer Research, The Affiliated Cancer Hospital, Guangzhou Medical University, Guangzhou, 510095, China; State Key Laboratory of Respiratory Disease, Guangzhou, 510180, ChinaGuangzhou Institute of Cancer Research, The Affiliated Cancer Hospital, Guangzhou Medical University, Guangzhou, 510095, China; State Key Laboratory of Respiratory Disease, Guangzhou, 510180, ChinaGuangzhou Institute of Cancer Research, The Affiliated Cancer Hospital, Guangzhou Medical University, Guangzhou, 510095, China; State Key Laboratory of Respiratory Disease, Guangzhou, 510180, ChinaGuangzhou Institute of Cancer Research, The Affiliated Cancer Hospital, Guangzhou Medical University, Guangzhou, 510095, China; State Key Laboratory of Respiratory Disease, Guangzhou, 510180, ChinaGuangzhou Institute of Cancer Research, The Affiliated Cancer Hospital, Guangzhou Medical University, Guangzhou, 510095, China; Corresponding author.Key Laboratory of Biomaterials of Guangdong Higher Education Institutes, Guangdong Provincial Engineering and Technological Research Center for Drug Carrier Development, Department of Biomedical Engineering, Jinan University, Guangzhou, 510632, China; Corresponding author.Guangzhou Institute of Cancer Research, The Affiliated Cancer Hospital, Guangzhou Medical University, Guangzhou, 510095, China; State Key Laboratory of Respiratory Disease, Guangzhou, 510180, China; Corresponding author. Guangzhou Institute of Cancer Research, The Affiliated Cancer Hospital, Guangzhou Medical University, Guangzhou, 510095, China.Immunotherapy resistance remains a substantial barrier to improving treatment outcomes for patients with lung adenocarcinoma (LUAD). Identifying effective immunotherapy target is crucial for enhancing therapeutic efficacy in LUAD. Through database analysis, we discovered that ADP ribosylhydrolase-like 1 (ADPRHL1, ARH2) is associated with immunosuppression. In this study, we first demonstrated that the increased presence of ARH2-positive macrophages in LUAD tumors is associated with immunosuppression. Furthermore, ARH2 promotes M2 macrophage polarization and suppresses immune responses by regulating the FPR2/PI3K/AKT signaling pathway. Additionally, we found that artesunate (ART) can induce necroptosis in LUAD cells and activate antitumor immune responses. To translate these findings into a clinically viable therapeutic approach, we developed a pH/ROS-responsive nanosystem capable of co-delivering siARH2 and ART. This nanosystem effectively activated immune responses in both tumor cells and tumor-associated macrophages. Furthermore, the nanosystem demonstrated excellent in vivo safety, precise PD-L1 targeting, and responsiveness to ROS and pH variations. It considerably suppressed the malignant phenotype of tumor cells induced by macrophages and enhanced T-cell-mediated immune responses. Overall, targeting ARH2 in combination with ART represents a promising novel strategy for the treatment of LUAD.http://www.sciencedirect.com/science/article/pii/S2452199X25003354ADP ribosylhydrolase-like 1 (ADPRHL1ARH2)Lung adenocarcinoma (LUAD)M2 macrophagesNecroptosispH/ROS-Responsive nanosystem
spellingShingle Rui Cai
Meng Wang
Mengting Pan
Zhiwu Zhang
Qiang Jia
Longbao Feng
Zhongjian Yu
Lu Liu
Tongyu Zhu
Silin Cai
Han Tian
Jiangyu Zhang
Rui Guo
Yanfang Zheng
Inhibition of ARH2 by pH/ROS-responsive nanosystem for improved lung adenocarcinoma immunochemotherapy
Bioactive Materials
ADP ribosylhydrolase-like 1 (ADPRHL1
ARH2)
Lung adenocarcinoma (LUAD)
M2 macrophages
Necroptosis
pH/ROS-Responsive nanosystem
title Inhibition of ARH2 by pH/ROS-responsive nanosystem for improved lung adenocarcinoma immunochemotherapy
title_full Inhibition of ARH2 by pH/ROS-responsive nanosystem for improved lung adenocarcinoma immunochemotherapy
title_fullStr Inhibition of ARH2 by pH/ROS-responsive nanosystem for improved lung adenocarcinoma immunochemotherapy
title_full_unstemmed Inhibition of ARH2 by pH/ROS-responsive nanosystem for improved lung adenocarcinoma immunochemotherapy
title_short Inhibition of ARH2 by pH/ROS-responsive nanosystem for improved lung adenocarcinoma immunochemotherapy
title_sort inhibition of arh2 by ph ros responsive nanosystem for improved lung adenocarcinoma immunochemotherapy
topic ADP ribosylhydrolase-like 1 (ADPRHL1
ARH2)
Lung adenocarcinoma (LUAD)
M2 macrophages
Necroptosis
pH/ROS-Responsive nanosystem
url http://www.sciencedirect.com/science/article/pii/S2452199X25003354
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