期刊
MOLECULES
卷 24, 期 15, 页码 -出版社
MDPI
DOI: 10.3390/molecules24152804
关键词
CA-170; PD-1; PD-L1; NMR; HTRF; immune checkpoint
资金
- Foundation for Polish Science - European Union under the European Regional Development Fund [POIR.04.04.00-00-420F/17-00]
- Foundation for Polish Science [TEAM TECH CORE FACILITY/2017-4/6]
CA-170 is currently the only small-molecule modulator in clinical trials targeting PD-L1 and VISTA proteins - important negative checkpoint regulators of immune activation. The reported therapeutic results to some extent mimic those of FDA-approved monoclonal antibodies overcoming the limitations of the high production costs and adverse effects of the latter. However, no conclusive biophysical evidence proving the binding to hPD-L1 has ever been presented. Using well-known in vitro methods: NMR binding assay, HTRF and cell-based activation assays, we clearly show that there is no direct binding between CA-170 and PD-L1. To strengthen our reasoning, we performed control experiments on AUNP-12 - a 29-mer peptide, which is a precursor of CA-170. Positive controls consisted of the well-documented small-molecule PD-L1 inhibitors: BMS-1166 and peptide-57.
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