凯发一触即发

至今,GenScript的服务及产品已被Cell, Nature, Science, PNAS等1300多家生物医药类杂志引用近万次,处于行业领先水平。NIH、哈佛、耶鲁、斯坦福、普林斯顿、杜克大学等约400家全球著名机构使用GenScript的基因合成、多肽服务、抗体服务和蛋白服务等成功地发表科研成果,再次证明GenScript 有能力帮助业内科学家Make research easy.

Discovery of a novel, potent and selective small-molecule inhibitor of PD-1/PD-L1 interaction with robust in vivo anti-tumour efficacy

Br J Pharmacol. 2021-03; 
Chenglong Liu, Feilong Zhou, Ziqin Yan, Lian Shen, Xichen Zhang, Fenglian He, Heng Wang, Xiaojie Lu, Ker Yu, Yujun Zhao, Di Zhu
Products/Services Used Details Operation
Recombinant Proteins … Biacore Assay hPD-L1(Genscript, Z03371), hPD-L2(Genscript, Z03417) or hPD-1 (Genscript, Z03370) were immobilized on a CM5 chip (GE Health) by using Biaocre T200. Page 15 … (Minneapolis, MN, USA). hPD-1, hPD-L1, and h-PD-L2 were from Genscript(Nanjing, China) … Get A Quote

摘要

objective: PD-1/PD-L1 antibodies have achieved great success in clinical treatment. However, monoclonal antibody drugs also have challenges, such as high manufacturing costs, poor diffusion, low oral bioavailability and limited penetration into tumour tissue. The development of small-molecule inhibitors of PD-1/PD-L1 interaction represents a promising perspective to overcome the above challenges in cancer immunotherapy. methods: We explored structural activity relationships and used biochemical assays to generate a lead compound (ZE132). CD8+ T-cells killing assay and Ifng expression assay were used to verify the in vitro cellular activity of ZE132. Off-target study was performed to verify the selectivity. Syng... More

关键词

PD-1/PD-L1, TGF-β, immunotherapy, tumour immune microenvironment