Characterization of the high-affinity anti-CTLA-4 monoclonal antibody JS007 for immune checkpoint therapy of cancer

Cytotoxic T lymphocyte-associated antigen 4 (CTLA-4) is a critical inhibitory checkpoint molecule, and monoclonal antibodies (mAbs) targeting CTLA-4 that restore anti-tumor T cell immunity have achieved clinical success. Here, we report a humanized IgG1 mAb, namely JS007, with high binding affinity...

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Main Authors: Jiawei Guan, Hongchuan Liu, Yan Chai, Jie Yu, Jian Yao, Jing Wang, Zhiwei Pan, Jing Zhang, Yuehua Zhou, Hui Liu, Sheng Yao, Jianxun Qi, Hui Feng, George F. Gao, Qihui Wang, Yi Shi, Shuguang Tan
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Sprog:engelsk
Udgivet: Taylor & Francis Group 2023-12-01
Serier:mAbs
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Online adgang:https://www.tandfonline.com/doi/10.1080/19420862.2022.2153409
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author Jiawei Guan
Hongchuan Liu
Yan Chai
Jie Yu
Jian Yao
Jing Wang
Zhiwei Pan
Jing Zhang
Yuehua Zhou
Hui Liu
Sheng Yao
Jianxun Qi
Hui Feng
George F. Gao
Qihui Wang
Yi Shi
Shuguang Tan
author_facet Jiawei Guan
Hongchuan Liu
Yan Chai
Jie Yu
Jian Yao
Jing Wang
Zhiwei Pan
Jing Zhang
Yuehua Zhou
Hui Liu
Sheng Yao
Jianxun Qi
Hui Feng
George F. Gao
Qihui Wang
Yi Shi
Shuguang Tan
author_sort Jiawei Guan
collection DOAJ
description Cytotoxic T lymphocyte-associated antigen 4 (CTLA-4) is a critical inhibitory checkpoint molecule, and monoclonal antibodies (mAbs) targeting CTLA-4 that restore anti-tumor T cell immunity have achieved clinical success. Here, we report a humanized IgG1 mAb, namely JS007, with high binding affinity to CTLA-4. JS007 shows superior binding affinity and T-cell activating efficiency over ipilimumab. Moreover, it demonstrates substantial in vivo tumor suppression efficacy at low doses. The crystal structure of JS007/CTLA-4 complex (PDB: 8HIT) shows JS007 adopts a heavy-chain-dominant binding mode, and mainly contacts the BC loop, DE loop and FG loop of CTLA-4. Notably, two Tyr residues (VH-Y100 and VL-Y32) from the complementarity-determining region loops insert into the two cavities formed by the residues from the loops of CTLA-4, which may contribute to the stabilization of the binding. Comparative analysis with other anti-CTLA-4 mAbs indicates that the double “wedge-into-hole” binding mode is unique for JS007 and may be responsible for the high-affinity binding to CTLA-4. These findings have provided an important molecular understanding of the high-affinity CTLA-4 blockade mAbs and shed light on future development of agents targeting CTLA-4.
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spelling doaj-art-a7f6d01c43cd47519759b8c736f474472025-07-23T08:11:25ZengTaylor & Francis GroupmAbs1942-08621942-08702023-12-0115110.1080/19420862.2022.2153409Characterization of the high-affinity anti-CTLA-4 monoclonal antibody JS007 for immune checkpoint therapy of cancerJiawei Guan0Hongchuan Liu1Yan Chai2Jie Yu3Jian Yao4Jing Wang5Zhiwei Pan6Jing Zhang7Yuehua Zhou8Hui Liu9Sheng Yao10Jianxun Qi11Hui Feng12George F. Gao13Qihui Wang14Yi Shi15Shuguang Tan16Key Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences (CAS), ChinaDepartment of Antibody Discovery and Engineering, Shanghai Junshi Biosciences Co Ltd, Shanghai, ChinaKey Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences (CAS), ChinaPilot National Laboratory for Marine Science and Technology (Qingdao), Shandong, ChinaDepartment of Antibody Discovery and Engineering, Shanghai Junshi Biosciences Co Ltd, Shanghai, ChinaDepartment of Antibody Discovery and Engineering, Shanghai Junshi Biosciences Co Ltd, Shanghai, ChinaDepartment of Antibody Discovery and Engineering, Shanghai Junshi Biosciences Co Ltd, Shanghai, ChinaDepartment of Antibody Discovery and Engineering, Shanghai Junshi Biosciences Co Ltd, Shanghai, ChinaDepartment of Antibody Discovery and Engineering, Shanghai Junshi Biosciences Co Ltd, Shanghai, ChinaDepartment of Antibody Discovery and Engineering, Shanghai Junshi Biosciences Co Ltd, Shanghai, ChinaDepartment of Antibody Discovery and Engineering, Shanghai Junshi Biosciences Co Ltd, Shanghai, ChinaKey Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences (CAS), ChinaDepartment of Antibody Discovery and Engineering, Shanghai Junshi Biosciences Co Ltd, Shanghai, ChinaKey Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences (CAS), ChinaKey Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences (CAS), ChinaKey Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences (CAS), ChinaKey Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences (CAS), ChinaCytotoxic T lymphocyte-associated antigen 4 (CTLA-4) is a critical inhibitory checkpoint molecule, and monoclonal antibodies (mAbs) targeting CTLA-4 that restore anti-tumor T cell immunity have achieved clinical success. Here, we report a humanized IgG1 mAb, namely JS007, with high binding affinity to CTLA-4. JS007 shows superior binding affinity and T-cell activating efficiency over ipilimumab. Moreover, it demonstrates substantial in vivo tumor suppression efficacy at low doses. The crystal structure of JS007/CTLA-4 complex (PDB: 8HIT) shows JS007 adopts a heavy-chain-dominant binding mode, and mainly contacts the BC loop, DE loop and FG loop of CTLA-4. Notably, two Tyr residues (VH-Y100 and VL-Y32) from the complementarity-determining region loops insert into the two cavities formed by the residues from the loops of CTLA-4, which may contribute to the stabilization of the binding. Comparative analysis with other anti-CTLA-4 mAbs indicates that the double “wedge-into-hole” binding mode is unique for JS007 and may be responsible for the high-affinity binding to CTLA-4. These findings have provided an important molecular understanding of the high-affinity CTLA-4 blockade mAbs and shed light on future development of agents targeting CTLA-4.https://www.tandfonline.com/doi/10.1080/19420862.2022.2153409CTLA-4antibodyhigh affinitystructureJS007
spellingShingle Jiawei Guan
Hongchuan Liu
Yan Chai
Jie Yu
Jian Yao
Jing Wang
Zhiwei Pan
Jing Zhang
Yuehua Zhou
Hui Liu
Sheng Yao
Jianxun Qi
Hui Feng
George F. Gao
Qihui Wang
Yi Shi
Shuguang Tan
Characterization of the high-affinity anti-CTLA-4 monoclonal antibody JS007 for immune checkpoint therapy of cancer
mAbs
CTLA-4
antibody
high affinity
structure
JS007
title Characterization of the high-affinity anti-CTLA-4 monoclonal antibody JS007 for immune checkpoint therapy of cancer
title_full Characterization of the high-affinity anti-CTLA-4 monoclonal antibody JS007 for immune checkpoint therapy of cancer
title_fullStr Characterization of the high-affinity anti-CTLA-4 monoclonal antibody JS007 for immune checkpoint therapy of cancer
title_full_unstemmed Characterization of the high-affinity anti-CTLA-4 monoclonal antibody JS007 for immune checkpoint therapy of cancer
title_short Characterization of the high-affinity anti-CTLA-4 monoclonal antibody JS007 for immune checkpoint therapy of cancer
title_sort characterization of the high affinity anti ctla 4 monoclonal antibody js007 for immune checkpoint therapy of cancer
topic CTLA-4
antibody
high affinity
structure
JS007
url https://www.tandfonline.com/doi/10.1080/19420862.2022.2153409
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