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Can I read Novel phthalimides regulating PD-1/PD-L1 interaction as potential immunotherapy agents on EtoBox?
Novel phthalimides regulating PD-1/PD-L1 interaction as potential immunotherapy agents by Chengliang Sun; Yao Cheng; Xiaojia Liu; Gefei Wang; Wenjian Min; Xiao Wang; Kai Yuan; Yi Hou; Jiaxing Li; Haolin Zhang; Haojie Dong; Liping Wang; Chenguang Lou; Yanze Sun; Xinmiao Yu; Hongbin Deng; Yibei Xiao; Peng Yang is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Novel phthalimides regulating PD-1/PD-L1 interaction as potential immunotherapy agents about?
Programmed cell death 1(PD-1)/programmed cell death ligand 1(PD-L1) have emerged as one of the most promising immune checkpoint targets for cancer immunotherapy. Despite the inherent advantages of small-molecule inhibitors over antibodies, the discovery of small-molecule inhibitors has fallen behind that of antibody drugs. Based on docking studies between small molecule inhibitor and PD-L1 protein, changing the chemical linker of inhibitor from a flexible chain to an aromatic ring may improve its binding capacity to PD-L1 protein, which was not reported before. A series of novel phthalimide derivatives from structure-based rational design was synthesized. **P39** was identified as the best inhibitor with promising activity, which not only inhibited PD-1/PD-L1 interaction (IC~50~ = 8.9 nmol/L), but also enhanced killing efficacy of immune cells on cancer cells. Co-crystal data demonstrated that **P39** induced the dimerization of PD-L1 proteins, thereby blocking the binding of PD-1/PD-L1. Moreover, **P39** exhibited a favorable safety profile with a LD~50~ > 5000 mg/kg and showed significant __in vivo__ antitumor activity through promoting CD8^+^ T cell activation. All these data su
Who reads Novel phthalimides regulating PD-1/PD-L1 interaction as potential immunotherapy agents?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Chengliang Sun; Yao Cheng; Xiaojia Liu; Gefei Wang; Wenjian Min; Xiao Wang; Kai Yuan; Yi Hou; Jiaxing Li; Haolin Zhang; Haojie Dong; Liping Wang; Chenguang Lou; Yanze Sun; Xinmiao Yu; Hongbin Deng; Yibei Xiao; Peng Yang
- Publisher
- Elsevier BV
- Published
- 2022
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)