Effects on imidazoacridinone C-1311 on the transcriptomic profile in prostate cancer cell depending on their AR status.. Effects on imidazoacridinone C-1311 on the transcriptomic profile in prostate cancer cell depending on their AR status.

Human prostate cancer cells, LNCaP (AR+) and DU-145 (AR-), were treated with C-1311 to identify the transcriptomic profile and functionally relevant androgen-dependent and independent genes using RNA sequencing. Overall design: We examined the anti-prostate cancer properties of imidazoacridinone, C-1311. Using RNAseq we showed for the first time that C-1311 is a promising agent that targets the androgen receptor pathway by blocking AR transcriptional activity and has potent efficacy towards prostate cancer cells.

我们采用C-1311处理人前列腺癌细胞系LNCaP（雄激素受体（androgen receptor，AR）阳性，AR+）与DU-145（AR阴性，AR-），并通过RNA测序分析转录组谱，以筛选与雄激素依赖及非雄激素依赖通路相关的功能基因。
整体实验设计：本研究考察了咪唑并吖啶酮类化合物C-1311的抗前列腺癌活性。通过RNA测序分析，我们首次证实C-1311是一种极具开发潜力的候选抗前列腺癌药物，其可通过阻断雄激素受体（AR）的转录活性靶向调控雄激素受体通路，并对前列腺癌细胞展现出强效抗肿瘤活性。