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Molecules
Volume 24
Issue 15
10.3390/molecules24152804
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Article

CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not?

by
Bogdan Musielak
1,
Justyna Kocik
1,
Lukasz Skalniak
1,
Katarzyna Magiera-Mularz
1,
Dominik Sala
1,
Miroslawa Czub
1,
Malgorzata Stec
2,
Maciej Siedlar
2,
Tad A. Holak
1 and
Jacek Plewka
1,*
1
Faculty of Chemistry, Jagiellonian University, Gronostajowa 2, 30-387 Krakow, Poland
2
Department of Clinical Immunology, Institute of Pediatrics, Jagiellonian University Medical College, Wielicka 265, 30-663 Krakow, Poland
*
Author to whom correspondence should be addressed.
Molecules 2019, 24(15), 2804; https://doi.org/10.3390/molecules24152804
Received: 1 July 2019 / Revised: 29 July 2019 / Accepted: 30 July 2019 / Published: 1 August 2019
(This article belongs to the Special Issue Recent Advances in Anticancer Drugs)
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Abstract

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. View Full-Text
Keywords: CA-170; PD-1/PD-L1; NMR; HTRF; immune checkpoint CA-170; PD-1/PD-L1; NMR; HTRF; immune checkpoint
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MDPI and ACS Style

Musielak, B.; Kocik, J.; Skalniak, L.; Magiera-Mularz, K.; Sala, D.; Czub, M.; Stec, M.; Siedlar, M.; Holak, T.A.; Plewka, J. CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? Molecules 2019, 24, 2804. https://doi.org/10.3390/molecules24152804

AMA Style

Musielak B, Kocik J, Skalniak L, Magiera-Mularz K, Sala D, Czub M, Stec M, Siedlar M, Holak TA, Plewka J. CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? Molecules. 2019; 24(15):2804. https://doi.org/10.3390/molecules24152804

Chicago/Turabian Style

Musielak, Bogdan, Justyna Kocik, Lukasz Skalniak, Katarzyna Magiera-Mularz, Dominik Sala, Miroslawa Czub, Malgorzata Stec, Maciej Siedlar, Tad A. Holak, and Jacek Plewka. 2019. "CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not?" Molecules 24, no. 15: 2804. https://doi.org/10.3390/molecules24152804

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