Enhancement of efferocytosis through biased FPR2 signaling attenuates intestinal inflammation

Abstract Efficient clearance of dying cells (efferocytosis) is an evolutionarily conserved process for tissue homeostasis. Genetic enhancement of efferocytosis exhibits therapeutic potential for inflammation resolution and tissue repair. However, pharmacological approaches to enhance efferocytosis r...

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Main Authors: Ming‐Yue Wu, Yun‐Jun Ge, Er‐Jin Wang, Qi‐Wen Liao, Zheng‐Yu Ren, Yang Yu, Guoyuan Zhu, Chun‐Ping Liu, Meng‐Ni Zhang, Huanxing Su, Han‐Ming Shen, Ye Chen, Lei Wang, Yi‐Tao Wang, Min Li, Zhaoxiang Bian, Jin Chai, Richard D Ye, Jia‐Hong Lu
Format: Article
Language:English
Published: Springer Nature 2023-11-01
Series:EMBO Molecular Medicine
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Online Access:https://doi.org/10.15252/emmm.202317815
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author Ming‐Yue Wu
Yun‐Jun Ge
Er‐Jin Wang
Qi‐Wen Liao
Zheng‐Yu Ren
Yang Yu
Guoyuan Zhu
Chun‐Ping Liu
Meng‐Ni Zhang
Huanxing Su
Han‐Ming Shen
Ye Chen
Lei Wang
Yi‐Tao Wang
Min Li
Zhaoxiang Bian
Jin Chai
Richard D Ye
Jia‐Hong Lu
author_facet Ming‐Yue Wu
Yun‐Jun Ge
Er‐Jin Wang
Qi‐Wen Liao
Zheng‐Yu Ren
Yang Yu
Guoyuan Zhu
Chun‐Ping Liu
Meng‐Ni Zhang
Huanxing Su
Han‐Ming Shen
Ye Chen
Lei Wang
Yi‐Tao Wang
Min Li
Zhaoxiang Bian
Jin Chai
Richard D Ye
Jia‐Hong Lu
author_sort Ming‐Yue Wu
collection DOAJ
description Abstract Efficient clearance of dying cells (efferocytosis) is an evolutionarily conserved process for tissue homeostasis. Genetic enhancement of efferocytosis exhibits therapeutic potential for inflammation resolution and tissue repair. However, pharmacological approaches to enhance efferocytosis remain sparse due to a lack of targets for modulation. Here, we report the identification of columbamine (COL) which enhances macrophage‐mediated efferocytosis and attenuates intestinal inflammation in a murine colitis model. COL enhances efferocytosis by promoting LC3‐associated phagocytosis (LAP), a non‐canonical form of autophagy. Transcriptome analysis and pharmacological characterization revealed that COL is a biased agonist that occupies a part of the ligand binding pocket of formyl peptide receptor 2 (FPR2), a G‐protein coupled receptor involved in inflammation regulation. Genetic ablation of the Fpr2 gene or treatment with an FPR2 antagonist abolishes COL‐induced efferocytosis, anti‐colitis activity and LAP. Taken together, our study identifies FPR2 as a potential target for modulating LC3‐associated efferocytosis to alleviate intestinal inflammation and highlights the therapeutic value of COL, a natural and biased agonist of FPR2, in the treatment of inflammatory bowel disease.
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spelling doaj-art-2a73d763915d475b830783a8ca0d9a892025-08-20T03:46:19ZengSpringer NatureEMBO Molecular Medicine1757-46761757-46842023-11-01151212210.15252/emmm.202317815Enhancement of efferocytosis through biased FPR2 signaling attenuates intestinal inflammationMing‐Yue Wu0Yun‐Jun Ge1Er‐Jin Wang2Qi‐Wen Liao3Zheng‐Yu Ren4Yang Yu5Guoyuan Zhu6Chun‐Ping Liu7Meng‐Ni Zhang8Huanxing Su9Han‐Ming Shen10Ye Chen11Lei Wang12Yi‐Tao Wang13Min Li14Zhaoxiang Bian15Jin Chai16Richard D Ye17Jia‐Hong Lu18State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of MacauKobilka Institute of Innovative Drug Discovery, School of Medicine, The Chinese University of Hong KongState Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of MacauKobilka Institute of Innovative Drug Discovery, School of Medicine, The Chinese University of Hong KongState Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of MacauEngineering Research Center of Cell and Therapeutic Antibody Medicine, Ministry of Education, School of Pharmacy, Shanghai Jiao Tong UniversityState Key Laboratory of Quality Research in Chinese Medicine, Macau Institute for Applied Research in Medicine and Health, Macau University of Science and TechnologyState Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of MacauDepartment of Gastroenterology, The First Affiliated Hospital (Southwest Hospital), Third Military Medical University (Army Medical University)State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of MacauFaculty of Health Sciences, University of MacauIntegrative Microecology Center, Department of Gastroenterology, Shenzhen Hospital, Southern Medical UniversityDepartment of Cardiovascular Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese MedicineState Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of MacauSchool of Chinese Medicine, Hong Kong Baptist UniversitySchool of Chinese Medicine, Hong Kong Baptist UniversityDepartment of Gastroenterology, The First Affiliated Hospital (Southwest Hospital), Third Military Medical University (Army Medical University)Kobilka Institute of Innovative Drug Discovery, School of Medicine, The Chinese University of Hong KongState Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of MacauAbstract Efficient clearance of dying cells (efferocytosis) is an evolutionarily conserved process for tissue homeostasis. Genetic enhancement of efferocytosis exhibits therapeutic potential for inflammation resolution and tissue repair. However, pharmacological approaches to enhance efferocytosis remain sparse due to a lack of targets for modulation. Here, we report the identification of columbamine (COL) which enhances macrophage‐mediated efferocytosis and attenuates intestinal inflammation in a murine colitis model. COL enhances efferocytosis by promoting LC3‐associated phagocytosis (LAP), a non‐canonical form of autophagy. Transcriptome analysis and pharmacological characterization revealed that COL is a biased agonist that occupies a part of the ligand binding pocket of formyl peptide receptor 2 (FPR2), a G‐protein coupled receptor involved in inflammation regulation. Genetic ablation of the Fpr2 gene or treatment with an FPR2 antagonist abolishes COL‐induced efferocytosis, anti‐colitis activity and LAP. Taken together, our study identifies FPR2 as a potential target for modulating LC3‐associated efferocytosis to alleviate intestinal inflammation and highlights the therapeutic value of COL, a natural and biased agonist of FPR2, in the treatment of inflammatory bowel disease.https://doi.org/10.15252/emmm.202317815columbamineFPR2inflammatory bowel diseaseLC3‐associated efferocytosis
spellingShingle Ming‐Yue Wu
Yun‐Jun Ge
Er‐Jin Wang
Qi‐Wen Liao
Zheng‐Yu Ren
Yang Yu
Guoyuan Zhu
Chun‐Ping Liu
Meng‐Ni Zhang
Huanxing Su
Han‐Ming Shen
Ye Chen
Lei Wang
Yi‐Tao Wang
Min Li
Zhaoxiang Bian
Jin Chai
Richard D Ye
Jia‐Hong Lu
Enhancement of efferocytosis through biased FPR2 signaling attenuates intestinal inflammation
EMBO Molecular Medicine
columbamine
FPR2
inflammatory bowel disease
LC3‐associated efferocytosis
title Enhancement of efferocytosis through biased FPR2 signaling attenuates intestinal inflammation
title_full Enhancement of efferocytosis through biased FPR2 signaling attenuates intestinal inflammation
title_fullStr Enhancement of efferocytosis through biased FPR2 signaling attenuates intestinal inflammation
title_full_unstemmed Enhancement of efferocytosis through biased FPR2 signaling attenuates intestinal inflammation
title_short Enhancement of efferocytosis through biased FPR2 signaling attenuates intestinal inflammation
title_sort enhancement of efferocytosis through biased fpr2 signaling attenuates intestinal inflammation
topic columbamine
FPR2
inflammatory bowel disease
LC3‐associated efferocytosis
url https://doi.org/10.15252/emmm.202317815
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