A novel kinase inhibitor ax-0085 inhibits interferon-γ-mediated induction of pd-l1 expression and promotes immune reaction to lung adenocarcinoma cells

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초록

In this study, we describe a novel kinase inhibitor AX-0085 which can suppress the induction of PD-L1 expression by Interferon-γ (IFN-γ) in lung adenocarcinoma (LUAD) cells. AX-0085 effectively blocks JAK2/STAT1 signaling initiated by IFN-γ treatment and prevents nuclear localization of STAT1. Importantly, we demonstrate that AX-0085 reverses the IFN-γ-mediated repression of T cell activation in vitro and enhances the anti-tumor activity of anti-PD-1 antibody in vivo when used in combination. Finally, transcriptomic analyses indicated that AX-0085 is highly specific in targeting the IFN-γ-pathway, thereby raising the possibility of applying this reagent in combination therapy with checkpoint inhibitor antibodies. It may be particularly relevant in cases in which PD-L1-mediated T cell exhaustion leads to immunoevasive phenotypes.

키워드

AX-0085Cancer immunotherapyImmune checkpointLung adenocarcinomaPD-L1gamma interferonimmune checkpoint inhibitorJanus kinase 2phosphotransferase inhibitorprogrammed death 1 ligand 1STAT1 proteinanimal cellanimal experimentanimal modelanimal tissueantineoplastic activityArticlecancer immunotherapycell culturecoculturecombination drug therapycontrolled studycytokine productiondown regulationenzyme linked immunosorbent assaygene expressiongenetic transfectionhumanhuman cellhuman tissueimmunityimmunoblottingimmunocytochemistryimmunofluorescence assayJAK-STAT signalinglung adenocarcinoma cell linemousemRNA expression levelnonhumanprotein expressionprotein phosphorylationreal time polymerase chain reactionRNA extractionRNA sequencingT lymphocyte activationtranscriptomicstumor growthtumor xenografttype II interferon signalingupregulation
제목
A novel kinase inhibitor ax-0085 inhibits interferon-γ-mediated induction of pd-l1 expression and promotes immune reaction to lung adenocarcinoma cells
저자
Kim, JusongJang, HaeyeonLee, Gyu JinHur, YelimKeum, JuheeJo, Jung KiYun, Si-EunPark, Sung JunPark, Young JunChoi, Myeong JunKim, Kye-SeongKim, Jaesang
DOI
10.3390/cells11010019
발행일
2022-01
유형
Article
저널명
Cells
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