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Russomanno, Pasquale; Assoni, Giulia; Amato, Jussara; D’Amore, Vincenzo Maria; Scaglia, Riccardo; Brancaccio, Diego; Pedrini, Martina; Polcaro, Giovanna; La Pietra, Valeria; Orlando, Paolo; Falzoni, Marianna; Cerofolini, Linda; Giuntini, Stefano; Fragai, Marco; Pagano, Bruno; Donati, Greta; Novellino, Ettore; Quintavalle, Cristina; Condorelli, Gerolama; Sabbatino, Francesco; Seneci, Pierfausto; Arosio, Daniela; Pepe, Stefano; Marinelli, Luciana
Journal of medicinal chemistry, 11/2021, Letnik: 64, Številka: 21Journal Article
The inhibition of the PD-1/PD-L1 axis by monoclonal antibodies has achieved remarkable success in treating a growing number of cancers. However, a novel class of small organic molecules, with BMS-202 (1) as the lead, is emerging as direct PD-L1 inhibitors. Herein, we report a series of 2,4,6-tri- and 2,4-disubstituted 1,3,5-triazines, which were synthesized and assayed for their PD-L1 binding by NMR and homogeneous time-resolved fluorescence. Among them, compound 10 demonstrated to strongly bind with the PD-L1 protein and challenged it in a co-culture of PD-L1 expressing cancer cells (PC9 and HCC827 cells) and peripheral blood mononuclear cells enhanced antitumor immune activity of the latter. Compound 10 significantly increased interferon γ release and apoptotic induction of cancer cells, with low cytotoxicity in healthy cells when compared to 1, thus paving the way for subsequent preclinical optimization and medical applications.
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Dostop do baze podatkov JCR je dovoljen samo uporabnikom iz Slovenije. Vaš trenutni IP-naslov ni na seznamu dovoljenih za dostop, zato je potrebna avtentikacija z ustreznim računom AAI.
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Vir: Osebne bibliografije
in: SICRIS
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