PD-1/PD-L1 inhibitor 2 is a small-molecule PD-1/PD-L1 interaction inhibitor with an IC 50 of 18 nM. Biophysical studies demonstrate that BMS202 binds directly to PD-L1.\xa0Binding of BMS202 promotes PD-L1 dimerisation and blocks the PD-L1/ PD1 interaction
1.Ruoxia Wu, Jiaqing Xiong, Ting Zhou, Zhen Zhang, Zhen Huang, Sha Tian, Yongli Wang. (2023) Quercetin/Anti-PD-1 Antibody Combination Therapy Regulates the Gut Microbiota, Impacts Macrophage Immunity and Reshapes the Hepatocellular Carcinoma Tumor Microenvironment. Frontiers in Bioscience-Landmark, 28 (12):(327). [PMID:38179731][10.31083/j.fbl2812327]
2.Qiuyang Huang, Xiaoling Zang, Zhiwei Zhang, Hang Yu, Baoyan Ding, Zhuangzhuang Li, Simin Cheng, Xin Zhang, Mustafa R.K. Ali, Xue Qiu, Zhihua Lv. (2023) Study on endogenous inhibitors against PD-L1: cAMP as a potential candidate. INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES, 230 (123266). [PMID:36646351][10.1016/j.ijbiomac.2023.123266]
3.OuYang Y, Gao J, Zhao L, Lu J, Zhong H, Tang H, Jin S, Yue L, Li Y, Guo W, Xu Q, Lai Y.. (2021) Design, Synthesis, and Evaluation of o-(Biphenyl-3-ylmethoxy)nitrophenyl Derivatives as PD-1/PD-L1 Inhibitors with Potent Anticancer Efficacy In Vivo.. J Med Chem, 64 (11.0):(7646-7666). [PMID:34037385][10.1021/acs.jmedchem.1c00370]
References
1.Zak KM, Grudnik P, Guzik K, Zieba BJ, Musielak B, Dömling A, Dubin G, Holak TA. (2016) Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1).. Oncotarget, 7 (21):(30323-35). [PMID:27083005][10.1021/op500134e]
2.Al-Asmakh M et al.. (2021) Dasatinib and PD-L1 inhibitors provoke toxicity and inhibit angiogenesis in the embryo.. Biomed Pharmacother, 134 (111134). [PMID:33341672]
3.Ruoxia Wu, Jiaqing Xiong, Ting Zhou, Zhen Zhang, Zhen Huang, Sha Tian, Yongli Wang. (2023) Quercetin/Anti-PD-1 Antibody Combination Therapy Regulates the Gut Microbiota, Impacts Macrophage Immunity and Reshapes the Hepatocellular Carcinoma Tumor Microenvironment. Frontiers in Bioscience-Landmark, 28 (12):(327). [PMID:38179731][10.31083/j.fbl2812327]
4.Qiuyang Huang, Xiaoling Zang, Zhiwei Zhang, Hang Yu, Baoyan Ding, Zhuangzhuang Li, Simin Cheng, Xin Zhang, Mustafa R.K. Ali, Xue Qiu, Zhihua Lv. (2023) Study on endogenous inhibitors against PD-L1: cAMP as a potential candidate. INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES, 230 (123266). [PMID:36646351][10.1016/j.ijbiomac.2023.123266]
5.OuYang Y, Gao J, Zhao L, Lu J, Zhong H, Tang H, Jin S, Yue L, Li Y, Guo W, Xu Q, Lai Y.. (2021) Design, Synthesis, and Evaluation of o-(Biphenyl-3-ylmethoxy)nitrophenyl Derivatives as PD-1/PD-L1 Inhibitors with Potent Anticancer Efficacy In Vivo.. J Med Chem, 64 (11.0):(7646-7666). [PMID:34037385][10.1021/acs.jmedchem.1c00370]
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H2217200