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Can I read Identification of a novel small-molecule inhibitor targeting TIM-3 for cancer immunotherapy on EtoBox?
Identification of a novel small-molecule inhibitor targeting TIM-3 for cancer immunotherapy by Menghan Wu; Aijun Wu; Xiangrui Zhang; Yang Li; Beibei Li; Shengzhe Jin; Qingyu Dong; Xiaoshuang Niu; Lihan Zhang; Xiaowen Zhou; Jiangfeng Du; Yahong Wu; Wenjie Zhai; Xiuman Zhou; Lu Qiu; Yanfeng Gao; Wenshan Zhao is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Identification of a novel small-molecule inhibitor targeting TIM-3 for cancer immunotherapy about?
PD-1/PD-L1 blockade has achieved substantial clinical results in cancer treatment. However, the expression of other immune checkpoints leads to resistance and hinders the efficacy of PD-1/PD-L1 blockade. T cell immunoglobulin and mucin domain 3 (TIM-3), a non-redundant immune checkpoint, synergizes with PD-1 to mediate T cell dysfunction in tumor microenvironment. Development of small molecules targeting TIM-3 is a promising strategy for cancer immunotherapy. Here, to identify small molecule inhibitors targeting TIM-3, the docking pocket in TIM-3 was analyzed by Molecular Operating Environment (MOE) and the Chemdiv compound database was screened. The small molecule SMI402 could bind to TIM-3 with high affinity and prevent the ligation of PtdSer, HMGB1, and CEACAM1. SMI402 reinvigorated T cell function in vitro. In the MC38-bearing mouse model, SMI402 inhibited tumor growth by increasing CD8+ T and natural killing (NK) cells infiltration at the tumor site, as well as restoring the function of CD8+ T and NK cells. In conclusions, the small molecule SMI402 shows promise as a leading compound which targets TIM-3 for cancer immunotherapy.
Who reads Identification of a novel small-molecule inhibitor targeting TIM-3 for cancer immunotherapy?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Menghan Wu; Aijun Wu; Xiangrui Zhang; Yang Li; Beibei Li; Shengzhe Jin; Qingyu Dong; Xiaoshuang Niu; Lihan Zhang; Xiaowen Zhou; Jiangfeng Du; Yahong Wu; Wenjie Zhai; Xiuman Zhou; Lu Qiu; Yanfeng Gao; Wenshan Zhao
- Publisher
- Elsevier BV
- Published
- 2023
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)