小分子
化学
单克隆抗体
免疫疗法
程序性细胞死亡
细胞凋亡
药物发现
癌症免疫疗法
药理学
癌症研究
癌症
抗体
生物化学
免疫学
医学
内科学
作者
Tianyu Wang,Xiaoxing Wu,Cui Guo,Kuojun Zhang,Jinyi Xu,Zheng Li,Sheng Jiang
标识
DOI:10.1021/acs.jmedchem.8b00990
摘要
The clinical success of inhibitors targeting the PD-1/PD-L1 pathway has made this an active field in cancer immunotherapy. Currently, most drugs targeting this pathway are monoclonal antibodies. Small-molecule inhibitors as the alternative to monoclonal antibodies are expected to overcome the disadvantages of mAbs which include production difficulties and their long half-life. Recently, progress has been reported on anti-PD-1/PD-L1 small-molecule inhibitors. In this paper, we review the development of inhibitors targeting the PD-1/PD-L1 pathway, focusing mainly on peptide-based and nonpeptidic small-molecule inhibitors. The structures and the preclinical and clinical studies of several peptide-based small-molecule candidate compounds in clinical trials are discussed. We also illustrate the design strategies underlying reported nonpeptidic small-molecule inhibitors and provide insight into possible future exploration. Development of small-molecule drugs for anti-PD-1/PD-L1 activity with specific cancer applications is a promising and challenging prospect.
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