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| author_facet |
Musielak, Bogdan Kocik, Justyna Skalniak, Lukasz Magiera-Mularz, Katarzyna Sala, Dominik Czub, Miroslawa Stec, Malgorzata Siedlar, Maciej Holak, Tad A. Plewka, Jacek Musielak, Bogdan Kocik, Justyna Skalniak, Lukasz Magiera-Mularz, Katarzyna Sala, Dominik Czub, Miroslawa Stec, Malgorzata Siedlar, Maciej Holak, Tad A. Plewka, Jacek |
|---|---|
| author |
Musielak, Bogdan Kocik, Justyna Skalniak, Lukasz Magiera-Mularz, Katarzyna Sala, Dominik Czub, Miroslawa Stec, Malgorzata Siedlar, Maciej Holak, Tad A. Plewka, Jacek |
| spellingShingle |
Musielak, Bogdan Kocik, Justyna Skalniak, Lukasz Magiera-Mularz, Katarzyna Sala, Dominik Czub, Miroslawa Stec, Malgorzata Siedlar, Maciej Holak, Tad A. Plewka, Jacek Molecules CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? Chemistry (miscellaneous) Analytical Chemistry Organic Chemistry Physical and Theoretical Chemistry Molecular Medicine Drug Discovery Pharmaceutical Science |
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musielak, bogdan |
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Musielak, Bogdan Kocik, Justyna Skalniak, Lukasz Magiera-Mularz, Katarzyna Sala, Dominik Czub, Miroslawa Stec, Malgorzata Siedlar, Maciej Holak, Tad A. Plewka, Jacek 1420-3049 MDPI AG Chemistry (miscellaneous) Analytical Chemistry Organic Chemistry Physical and Theoretical Chemistry Molecular Medicine Drug Discovery Pharmaceutical Science http://dx.doi.org/10.3390/molecules24152804 <jats:p>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.</jats:p> CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? Molecules |
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| title |
CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? |
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CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? |
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CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? |
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CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? |
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CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? |
| title_short |
CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? |
| title_sort |
ca-170 – a potent small-molecule pd-l1 inhibitor or not? |
| topic |
Chemistry (miscellaneous) Analytical Chemistry Organic Chemistry Physical and Theoretical Chemistry Molecular Medicine Drug Discovery Pharmaceutical Science |
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http://dx.doi.org/10.3390/molecules24152804 |
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2019 |
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<jats:p>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.</jats:p> |
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| author | Musielak, Bogdan, Kocik, Justyna, Skalniak, Lukasz, Magiera-Mularz, Katarzyna, Sala, Dominik, Czub, Miroslawa, Stec, Malgorzata, Siedlar, Maciej, Holak, Tad A., Plewka, Jacek |
| author_facet | Musielak, Bogdan, Kocik, Justyna, Skalniak, Lukasz, Magiera-Mularz, Katarzyna, Sala, Dominik, Czub, Miroslawa, Stec, Malgorzata, Siedlar, Maciej, Holak, Tad A., Plewka, Jacek, Musielak, Bogdan, Kocik, Justyna, Skalniak, Lukasz, Magiera-Mularz, Katarzyna, Sala, Dominik, Czub, Miroslawa, Stec, Malgorzata, Siedlar, Maciej, Holak, Tad A., Plewka, Jacek |
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| description | <jats:p>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.</jats:p> |
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| spelling | Musielak, Bogdan Kocik, Justyna Skalniak, Lukasz Magiera-Mularz, Katarzyna Sala, Dominik Czub, Miroslawa Stec, Malgorzata Siedlar, Maciej Holak, Tad A. Plewka, Jacek 1420-3049 MDPI AG Chemistry (miscellaneous) Analytical Chemistry Organic Chemistry Physical and Theoretical Chemistry Molecular Medicine Drug Discovery Pharmaceutical Science http://dx.doi.org/10.3390/molecules24152804 <jats:p>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.</jats:p> CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? Molecules |
| spellingShingle | Musielak, Bogdan, Kocik, Justyna, Skalniak, Lukasz, Magiera-Mularz, Katarzyna, Sala, Dominik, Czub, Miroslawa, Stec, Malgorzata, Siedlar, Maciej, Holak, Tad A., Plewka, Jacek, Molecules, CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not?, Chemistry (miscellaneous), Analytical Chemistry, Organic Chemistry, Physical and Theoretical Chemistry, Molecular Medicine, Drug Discovery, Pharmaceutical Science |
| title | CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? |
| title_full | CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? |
| title_fullStr | CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? |
| title_full_unstemmed | CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? |
| title_short | CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? |
| title_sort | ca-170 – a potent small-molecule pd-l1 inhibitor or not? |
| title_unstemmed | CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not? |
| topic | Chemistry (miscellaneous), Analytical Chemistry, Organic Chemistry, Physical and Theoretical Chemistry, Molecular Medicine, Drug Discovery, Pharmaceutical Science |
| url | http://dx.doi.org/10.3390/molecules24152804 |