Citrullination of NF‐κB p65 by PAD2 as a Novel Therapeutic Target for Modulating Macrophage Polarization in Acute Lung Injury

Abstract Mediating protein citrullination, peptidyl arginine deiminase 2 (PAD2) has recently been reported to influence macrophage phenotypes. However, the mechanisms of PAD2 on macrophage function in Pseudomonas aeruginosa (PA)‐induced acute lung injury syndrome (ALI) remains unclear. Utilizing sin...

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Main Authors: Xin Yu, Yujing Song, Tao Dong, Wenlu Ouyang, Chao Quan, Liujiazi Shao, Leonard Barasa, Paul R. Thompson, Mao Zhang, Jianjie Ma, Katsuo Kurabayashi, Yongqing Li
Format: Article
Language:English
Published: Wiley 2025-05-01
Series:Advanced Science
Subjects:
Online Access:https://doi.org/10.1002/advs.202413253
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author Xin Yu
Yujing Song
Tao Dong
Wenlu Ouyang
Chao Quan
Liujiazi Shao
Leonard Barasa
Paul R. Thompson
Mao Zhang
Jianjie Ma
Katsuo Kurabayashi
Yongqing Li
author_facet Xin Yu
Yujing Song
Tao Dong
Wenlu Ouyang
Chao Quan
Liujiazi Shao
Leonard Barasa
Paul R. Thompson
Mao Zhang
Jianjie Ma
Katsuo Kurabayashi
Yongqing Li
author_sort Xin Yu
collection DOAJ
description Abstract Mediating protein citrullination, peptidyl arginine deiminase 2 (PAD2) has recently been reported to influence macrophage phenotypes. However, the mechanisms of PAD2 on macrophage function in Pseudomonas aeruginosa (PA)‐induced acute lung injury syndrome (ALI) remains unclear. Utilizing single‐cell RNA sequencing and mass spectrometry‐based proteomics, a new citrullination site at arginine 171 (R171) is discovered within nuclear factor‐ κB (NF‐κB) p65 catalyzed by PAD2, which modulates PAD2‐NF‐κB p65‐importin α3 pathway and its downstream M1/M2 macrophage polarization. Building on these findings, a cell‐specific targeted therapeutic strategy using gold nanoparticles (AuNPs) conjugated with a novel PAD2 inhibitor, AFM41a, and an intercellular adhesion molecule‐1 (ICAM‐1) antibody is developed. This approach enables the selective delivery of the inhibitor to M1‐polarized macrophages in the PA‐infected alveolar niche. In vivo, this nanomedicine reduces excessive inflammation and promotes M1‐to‐M2 polarization to inhibit ALI. This study highlights the role of PAD2‐mediated citrullination in macrophage polarization and introduces a promising nanoparticle‐based therapy for PA‐induced ALI.
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spelling doaj-art-31f04a8b77b548c0b6cb2dbeef8be2b32025-08-20T02:34:47ZengWileyAdvanced Science2198-38442025-05-011218n/an/a10.1002/advs.202413253Citrullination of NF‐κB p65 by PAD2 as a Novel Therapeutic Target for Modulating Macrophage Polarization in Acute Lung InjuryXin Yu0Yujing Song1Tao Dong2Wenlu Ouyang3Chao Quan4Liujiazi Shao5Leonard Barasa6Paul R. Thompson7Mao Zhang8Jianjie Ma9Katsuo Kurabayashi10Yongqing Li11Department of Surgery University of Michigan Health System Ann Arbor MI 48109 USADepartment of Mechanical and Aerospace Engineering New York University Tandon School of Engineering Brooklyn NY 11201 USADepartment of Surgery University of Michigan Health System Ann Arbor MI 48109 USADepartment of Surgery University of Michigan Health System Ann Arbor MI 48109 USADepartment of Surgery University of Michigan Health System Ann Arbor MI 48109 USADepartment of Surgery University of Michigan Health System Ann Arbor MI 48109 USAProgram in Chemical Biology, Department of Biochemistry and Molecular Biotechnology University of Massachusetts Chan Medical School Worcester MA 01605 USAProgram in Chemical Biology, Department of Biochemistry and Molecular Biotechnology University of Massachusetts Chan Medical School Worcester MA 01605 USADepartment of Emergency Medicine Second Affiliated Hospital Zhejiang University School of Medicine No.88 Jiefang Road Hangzhou Zhejiang 310009 ChinaDepartment of Surgery Division of Surgical Science University of Virginia Charlottesville VA 22903 USADepartment of Mechanical and Aerospace Engineering New York University Tandon School of Engineering Brooklyn NY 11201 USADepartment of Surgery University of Michigan Health System Ann Arbor MI 48109 USAAbstract Mediating protein citrullination, peptidyl arginine deiminase 2 (PAD2) has recently been reported to influence macrophage phenotypes. However, the mechanisms of PAD2 on macrophage function in Pseudomonas aeruginosa (PA)‐induced acute lung injury syndrome (ALI) remains unclear. Utilizing single‐cell RNA sequencing and mass spectrometry‐based proteomics, a new citrullination site at arginine 171 (R171) is discovered within nuclear factor‐ κB (NF‐κB) p65 catalyzed by PAD2, which modulates PAD2‐NF‐κB p65‐importin α3 pathway and its downstream M1/M2 macrophage polarization. Building on these findings, a cell‐specific targeted therapeutic strategy using gold nanoparticles (AuNPs) conjugated with a novel PAD2 inhibitor, AFM41a, and an intercellular adhesion molecule‐1 (ICAM‐1) antibody is developed. This approach enables the selective delivery of the inhibitor to M1‐polarized macrophages in the PA‐infected alveolar niche. In vivo, this nanomedicine reduces excessive inflammation and promotes M1‐to‐M2 polarization to inhibit ALI. This study highlights the role of PAD2‐mediated citrullination in macrophage polarization and introduces a promising nanoparticle‐based therapy for PA‐induced ALI.https://doi.org/10.1002/advs.202413253acute lung injurygold nanoparticlesICAM‐1macrophage polarizationNF‐κB p65PAD2
spellingShingle Xin Yu
Yujing Song
Tao Dong
Wenlu Ouyang
Chao Quan
Liujiazi Shao
Leonard Barasa
Paul R. Thompson
Mao Zhang
Jianjie Ma
Katsuo Kurabayashi
Yongqing Li
Citrullination of NF‐κB p65 by PAD2 as a Novel Therapeutic Target for Modulating Macrophage Polarization in Acute Lung Injury
Advanced Science
acute lung injury
gold nanoparticles
ICAM‐1
macrophage polarization
NF‐κB p65
PAD2
title Citrullination of NF‐κB p65 by PAD2 as a Novel Therapeutic Target for Modulating Macrophage Polarization in Acute Lung Injury
title_full Citrullination of NF‐κB p65 by PAD2 as a Novel Therapeutic Target for Modulating Macrophage Polarization in Acute Lung Injury
title_fullStr Citrullination of NF‐κB p65 by PAD2 as a Novel Therapeutic Target for Modulating Macrophage Polarization in Acute Lung Injury
title_full_unstemmed Citrullination of NF‐κB p65 by PAD2 as a Novel Therapeutic Target for Modulating Macrophage Polarization in Acute Lung Injury
title_short Citrullination of NF‐κB p65 by PAD2 as a Novel Therapeutic Target for Modulating Macrophage Polarization in Acute Lung Injury
title_sort citrullination of nf κb p65 by pad2 as a novel therapeutic target for modulating macrophage polarization in acute lung injury
topic acute lung injury
gold nanoparticles
ICAM‐1
macrophage polarization
NF‐κB p65
PAD2
url https://doi.org/10.1002/advs.202413253
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