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Ai-fu Lin


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Journal of Zhejiang University SCIENCE B 2022 Vol.23 No.10 P.823-843


Tumor immune checkpoints and their associated inhibitors

Author(s):  Zerui GAO, Xingyi LING, Chengyu SHI, Ying WANG, Aifu LIN

Affiliation(s):  MOE Laboratory of Biosystem Homeostasis and Protection, College of Life Sciences, Zhejiang University, Hangzhou 310058, China; more

Corresponding email(s):   linaifu@zju.edu.cn

Key Words:  Immune checkpoint, Immune checkpoint inhibitor, Programmed cell death-ligand 1 (PD-L1), Cytotoxic T-lymphocyte-associated antigen-4 (CTLA-4), Lymphocyte activation gene-3 (LAG-3), T-cell immunoglobulin and immunoreceptor tyrosine-based inhibitory motif (ITIM) domain (TIGIT), B7 family

Zerui GAO, Xingyi LING, Chengyu SHI, Ying WANG, Aifu LIN. Tumor immune checkpoints and their associated inhibitors[J]. Journal of Zhejiang University Science B, 2022, 23(10): 823-843.

@article{title="Tumor immune checkpoints and their associated inhibitors",
author="Zerui GAO, Xingyi LING, Chengyu SHI, Ying WANG, Aifu LIN",
journal="Journal of Zhejiang University Science B",
publisher="Zhejiang University Press & Springer",

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%T Tumor immune checkpoints and their associated inhibitors
%A Zerui GAO
%A Xingyi LING
%A Chengyu SHI
%A Ying WANG
%A Aifu LIN
%J Journal of Zhejiang University SCIENCE B
%V 23
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%P 823-843
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%D 2022
%I Zhejiang University Press & Springer
%DOI 10.1631/jzus.B2200195

T1 - Tumor immune checkpoints and their associated inhibitors
A1 - Zerui GAO
A1 - Xingyi LING
A1 - Chengyu SHI
A1 - Ying WANG
A1 - Aifu LIN
J0 - Journal of Zhejiang University Science B
VL - 23
IS - 10
SP - 823
EP - 843
%@ 1673-1581
Y1 - 2022
PB - Zhejiang University Press & Springer
ER -
DOI - 10.1631/jzus.B2200195

Immunological evasion is one of the defining characteristics of cancers, as the immune modification of an immune checkpoint (IC) confers immune evasion capabilities to tumor cells. Multiple ICs, such as programmed cell death protein-1 (PD-1) and cytotoxic T-lymphocyte-associated antigen-4 (CTLA-4), can bind to their respective receptors and reduce tumor immunity in a variety of ways, including blocking immune cell activation signals. IC blockade (ICB) therapies targeting these checkpoint molecules have demonstrated significant clinical benefits. This is because antibody-based IC inhibitors and a variety of specific small molecule inhibitors can inhibit key oncogenic signaling pathways and induce durable tumor remission in patients with a variety of cancers. Deciphering the roles and regulatory mechanisms of these IC molecules will provide crucial theoretical guidance for clinical treatment. In this review, we summarize the current knowledge on the functional and regulatory mechanisms of these IC molecules at multiple levels, including epigenetic regulation, transcriptional regulation, and post-translational modifications. In addition, we provide a summary of the medications targeting various nodes in the regulatory pathway, and highlight the potential of newly identified IC molecules, focusing on their potential implications for cancer diagnostics and immunotherapy.




Darkslateblue:Affiliate; Royal Blue:Author; Turquoise:Article


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