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Abstract
Naphthyridine derivatives are a widely-used class of heterocycles due to their pharmacological activities. A novel compound (10-Methoxy-1,2,3,4-tetrahydrobenzo(g)(1,3) diazepino(1,2-a)-(1,8)naphthyridin-6-yl)(phenyl) methanone (named 3u), showed good anticancer activity in the human malignant melanoma cell line A375 via Thiazolyl Blue Tetrazolium Bromide (MTT) assay. After Western blotting confirmed, we found that 3u induces necroptosis at low concentrations and apoptosis at high concentrations via the upregulation of death receptors and scaffold protein in A375 cells. Furthermore, by combining 3u with the caspase inhibitor zVAD-fmk or Receptor Interacting Serine/Threonine Kinase 1 (RIP1) kinase inhibitor Necrostatin-1 (Nec-1), we found that the activity of caspase-8 was the crucial factor that determined whether either apoptosis or necroptosis occurred. The results indicate that 3u should be considered as a potential chemical substance for melanoma treatment.
Highlights
Melanoma is a disease besetting human beings for several centuries, and it has been documented in the literature since the 1600s [1]
We found checked whether A375 cells triggered caspase-3 dependent apoptosis by 3u treatment
death receptors (DRs) and adaptor proteins were upregulated in the that low concentrations of 3u triggered necroptosis, which led to cell death in A375 cells.treatments
Summary
Melanoma is a disease besetting human beings for several centuries, and it has been documented in the literature since the 1600s [1]. The extrinsic pathway initiated by the binding or activating of receptorsmitochondrial (DRs) of the tumor necrosis factor (TNF). Receptoris superfamily such as TNFR1, Fas, DR4, death receptors (DRs) of the tumor necrosis factor receptor superfamily such as TNFR1, Fas, and DR5 with their extracellular ligands or drugs This process is followed by the assembly of the DR4, and DR5 with their extracellular or drugs. Fas-associated via deathby domain protein of the death-inducing signal complex (DISC), which contains the. Necrosis is stereotyped as a form of cell death occurring in an manner as ainhibition result of adverse conditions. Death receptors can of trigger necrosis upon of apoptosis by a caspase inhibitor,conventional zVAD-fmk [17]. Decision between cell FADD, death via apoptosis or necroptosis assemble together with death receptors. Figure 1) showed good anticancer activity in human malignant melanoma cell line A375.
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