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  3. PD-1/PD-L1 inhibitor screening of caffeoylquinic acid compounds using surface plasmon resonance spectroscopy

PD-1/PD-L1 inhibitor screening of caffeoylquinic acid compounds using surface plasmon resonance spectroscopy

  • Anal Biochem. 2018 Apr 15;547:52-56. doi: 10.1016/j.ab.2018.02.003.
Ya Han 1,  Yaning Gao 1,  Tian He 1,  Daidong Wang 1,  Ning Guo 1,  Xiaotian Zhang 1,  Shizhong Chen 2,  Hong Wang 3
Affiliations

Affiliations

  • 1 Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
  • 2 Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. Electronic address: chenshizhong66@163.com.
  • 3 Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. Electronic address: hw9505@bjmu.edu.cn.
PMID: 29428377 DOI: 10.1016/j.ab.2018.02.003
Abstract

Following the FDA approval of three monoclonal Antibodies of PD-1/PD-L1, this pathway has become a promising target for Cancer treatment. Currently small-molecule inhibitors have not been extensively investigated, and appropriate screening methods for such inhibitors are urgently required. In this study, surface plasmon resonance (SPR) technology was used to evaluate the affinity and competitive inhibition of nine caffeoylquinic acid compounds (CQAs) against PD-1/PD-L1. As a result, four small molecules including 1-CQA, 3-CQA, 4-CQA and 5-CQA were determined as PD-1/PD-L1 inhibitors. This study provided an efficient method for screening small-molecule inhibitors targeting PD-1/PD-L1 pathway.

Keywords

Caffeoylquinic acid compounds; PD-1; PD-L1; Small-molecule inhibitors; Surface plasmon resonance.

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