Dual blockade of IL-17A and IL-36 pathways via a bispecific antibody exhibits enhanced anti-inflammatory potency

Antibody drugs targeting single inflammatory cytokines have revolutionized the treatment of immune-mediated inflammatory diseases. To investigate whether dual targeting interleukin-17 (IL-17) and IL-36 enhances anti-inflammatory activity, bispecific Ab HB0043 was generated by linking the single chai...

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Main Authors: Xiaojuan Ma, Shuang Zhang, Xiaochen Ren, Yujie Feng, Hui Li, Shi Chen, Jingen Xu, Yanting Wang, Guo-yuan Peng, Qingran Yan, Huifeng Jia, Simin Xia, Xiaopei Cui, Xiaofang Chen, Xianfei Pan, Shaojie Wang, Haijia Yu, Xiaoyue Wei, Mingwei Li, Bei Liu, Jingyue Xu, Qiaoxia Qian, Xiangyang Zhu, Yifan Zhan, Liangjing Lu
Format: Article
Language:English
Published: Frontiers Media S.A. 2024-11-01
Series:Frontiers in Immunology
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Online Access:https://www.frontiersin.org/articles/10.3389/fimmu.2024.1434127/full
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author Xiaojuan Ma
Xiaojuan Ma
Shuang Zhang
Xiaochen Ren
Xiaochen Ren
Yujie Feng
Hui Li
Shi Chen
Jingen Xu
Yanting Wang
Guo-yuan Peng
Qingran Yan
Huifeng Jia
Simin Xia
Xiaopei Cui
Xiaofang Chen
Xianfei Pan
Shaojie Wang
Haijia Yu
Xiaoyue Wei
Mingwei Li
Bei Liu
Jingyue Xu
Qiaoxia Qian
Xiangyang Zhu
Yifan Zhan
Liangjing Lu
author_facet Xiaojuan Ma
Xiaojuan Ma
Shuang Zhang
Xiaochen Ren
Xiaochen Ren
Yujie Feng
Hui Li
Shi Chen
Jingen Xu
Yanting Wang
Guo-yuan Peng
Qingran Yan
Huifeng Jia
Simin Xia
Xiaopei Cui
Xiaofang Chen
Xianfei Pan
Shaojie Wang
Haijia Yu
Xiaoyue Wei
Mingwei Li
Bei Liu
Jingyue Xu
Qiaoxia Qian
Xiangyang Zhu
Yifan Zhan
Liangjing Lu
author_sort Xiaojuan Ma
collection DOAJ
description Antibody drugs targeting single inflammatory cytokines have revolutionized the treatment of immune-mediated inflammatory diseases. To investigate whether dual targeting interleukin-17 (IL-17) and IL-36 enhances anti-inflammatory activity, bispecific Ab HB0043 was generated by linking the single chain fragment variables (scFvs) from humanized anti-IL-36R antibody (HB0034) to the C-terminus of the heavy chain of anti-IL-17A IgG1 (HB0017) Fc using a flexible peptide linker. HB0043 largely maintained the binding affinities and biological activities of the two parent monoclonal antibodies (mAbs) in vitro. IL-17 and IL-36 cooperated to amplify the expression of pro-inflammatory and pro-fibrotic genes in normal human dermal fibroblasts (NHDF). However, HB0043 more effectively blocked IL-6 and IL-8 production in NHDF stimulated by IL-17A and IL-36 compared to two monoclonal antibodies. In a mouse model of Oxazolone (OXA)-induced atopic dermatitis and Imiquimod (IMQ)-induced skin inflammation, administration of both anti-IL17A mAb HB0017 and anti-mouse IL-36R surrogate antibody HB0034SA showed improved effectiveness in alleviating skin thickening and inflammation based on histological assessment. Further, in cynomolgus monkeys, HB0043 showed no enhanced target-related toxicity compared with the two parental mAbs in vivo and with a moderate increase in production of anti-drug antibodies. Together, dual blockade of IL-17A and IL-36R in the form of a bispecific antibody may have advantages in blocking the overlapping and non-overlapping functions of these two cytokines in skin inflammation that could not optimally be curtailed with single mAbs. In conclusion, as monotherapy may reach therapeutic celling for certain difficult-to-treat inflammatory and fibrotic diseases, dual targeting could potentially pave a way to combat these diseases.
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record_format Article
series Frontiers in Immunology
spelling doaj-art-e25db7dcba894a3da6c08a51ec9bda6c2024-11-12T13:47:33ZengFrontiers Media S.A.Frontiers in Immunology1664-32242024-11-011510.3389/fimmu.2024.14341271434127Dual blockade of IL-17A and IL-36 pathways via a bispecific antibody exhibits enhanced anti-inflammatory potencyXiaojuan Ma0Xiaojuan Ma1Shuang Zhang2Xiaochen Ren3Xiaochen Ren4Yujie Feng5Hui Li6Shi Chen7Jingen Xu8Yanting Wang9Guo-yuan Peng10Qingran Yan11Huifeng Jia12Simin Xia13Xiaopei Cui14Xiaofang Chen15Xianfei Pan16Shaojie Wang17Haijia Yu18Xiaoyue Wei19Mingwei Li20Bei Liu21Jingyue Xu22Qiaoxia Qian23Xiangyang Zhu24Yifan Zhan25Liangjing Lu26Rheumatology, Shanghai Jiao Tong University School of Medicine Affiliated Renji Hospital, Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Pharmacology, School of Pharmacy, Fudan University, Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaRheumatology, Shanghai Jiao Tong University School of Medicine Affiliated Renji Hospital, Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaRheumatology, Shanghai Jiao Tong University School of Medicine Affiliated Renji Hospital, Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaDepartment of Drug Discovery, Shanghai Huaota Biopharmaceutical Co. Ltd., Shanghai, ChinaRheumatology, Shanghai Jiao Tong University School of Medicine Affiliated Renji Hospital, Shanghai, ChinaAntibody drugs targeting single inflammatory cytokines have revolutionized the treatment of immune-mediated inflammatory diseases. To investigate whether dual targeting interleukin-17 (IL-17) and IL-36 enhances anti-inflammatory activity, bispecific Ab HB0043 was generated by linking the single chain fragment variables (scFvs) from humanized anti-IL-36R antibody (HB0034) to the C-terminus of the heavy chain of anti-IL-17A IgG1 (HB0017) Fc using a flexible peptide linker. HB0043 largely maintained the binding affinities and biological activities of the two parent monoclonal antibodies (mAbs) in vitro. IL-17 and IL-36 cooperated to amplify the expression of pro-inflammatory and pro-fibrotic genes in normal human dermal fibroblasts (NHDF). However, HB0043 more effectively blocked IL-6 and IL-8 production in NHDF stimulated by IL-17A and IL-36 compared to two monoclonal antibodies. In a mouse model of Oxazolone (OXA)-induced atopic dermatitis and Imiquimod (IMQ)-induced skin inflammation, administration of both anti-IL17A mAb HB0017 and anti-mouse IL-36R surrogate antibody HB0034SA showed improved effectiveness in alleviating skin thickening and inflammation based on histological assessment. Further, in cynomolgus monkeys, HB0043 showed no enhanced target-related toxicity compared with the two parental mAbs in vivo and with a moderate increase in production of anti-drug antibodies. Together, dual blockade of IL-17A and IL-36R in the form of a bispecific antibody may have advantages in blocking the overlapping and non-overlapping functions of these two cytokines in skin inflammation that could not optimally be curtailed with single mAbs. In conclusion, as monotherapy may reach therapeutic celling for certain difficult-to-treat inflammatory and fibrotic diseases, dual targeting could potentially pave a way to combat these diseases.https://www.frontiersin.org/articles/10.3389/fimmu.2024.1434127/fullbispecific antibodyIL-17AIL-36Rskin inflammationskin fibrosis
spellingShingle Xiaojuan Ma
Xiaojuan Ma
Shuang Zhang
Xiaochen Ren
Xiaochen Ren
Yujie Feng
Hui Li
Shi Chen
Jingen Xu
Yanting Wang
Guo-yuan Peng
Qingran Yan
Huifeng Jia
Simin Xia
Xiaopei Cui
Xiaofang Chen
Xianfei Pan
Shaojie Wang
Haijia Yu
Xiaoyue Wei
Mingwei Li
Bei Liu
Jingyue Xu
Qiaoxia Qian
Xiangyang Zhu
Yifan Zhan
Liangjing Lu
Dual blockade of IL-17A and IL-36 pathways via a bispecific antibody exhibits enhanced anti-inflammatory potency
Frontiers in Immunology
bispecific antibody
IL-17A
IL-36R
skin inflammation
skin fibrosis
title Dual blockade of IL-17A and IL-36 pathways via a bispecific antibody exhibits enhanced anti-inflammatory potency
title_full Dual blockade of IL-17A and IL-36 pathways via a bispecific antibody exhibits enhanced anti-inflammatory potency
title_fullStr Dual blockade of IL-17A and IL-36 pathways via a bispecific antibody exhibits enhanced anti-inflammatory potency
title_full_unstemmed Dual blockade of IL-17A and IL-36 pathways via a bispecific antibody exhibits enhanced anti-inflammatory potency
title_short Dual blockade of IL-17A and IL-36 pathways via a bispecific antibody exhibits enhanced anti-inflammatory potency
title_sort dual blockade of il 17a and il 36 pathways via a bispecific antibody exhibits enhanced anti inflammatory potency
topic bispecific antibody
IL-17A
IL-36R
skin inflammation
skin fibrosis
url https://www.frontiersin.org/articles/10.3389/fimmu.2024.1434127/full
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