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M344抑制神经母细胞瘤中组蛋白去乙酰化酶相关表型和肿瘤生长。

M344 Suppresses Histone Deacetylase-Associated Phenotypes and Tumor Growth in Neuroblastoma.

作者信息

Brumfield Gabrielle L, Doty Kenadie R, Knoche Shelby M, Larson Alaina C, Gephart Benjamin D, Coulter Don W, Solheim Joyce C

机构信息

Eppley Institute, University of Nebraska Medical Center, Omaha, NE 68198, USA.

Fred & Pamela Buffett Cancer Center, University of Nebraska Medical Center, Omaha, NE 68198, USA.

出版信息

Int J Mol Sci. 2025 Sep 1;26(17):8494. doi: 10.3390/ijms26178494.

Abstract

Neuroblastoma (NB) is an aggressive pediatric cancer, with high-risk patients facing a five-year survival rate of ~50%. Standard therapies, including surgery, chemotherapy, radiation, and immunotherapy, are associated with significant long-term toxicities and frequent relapse. Histone deacetylase (HDAC) inhibitors have emerged as promising agents for cancer therapy, given their role in modulating gene expression and tumor phenotypes. This study evaluated M344 [4-(dimethylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)benzamide], an HDAC inhibitor, for its efficacy and mechanisms of action against NB. Analysis of clinical NB Gene Expression Omnibus data revealed advanced-stage tumors exhibit higher HDAC expression relative to early-stage samples. M344 treatment effectively increased histone acetylation, induced G0/G1 cell cycle arrest, and activated caspase-mediated cell death. Relative to vorinostat, an HDAC inhibitor in clinical use for lymphoma and clinical trials for NB, M344 displayed superior cytostatic, cytotoxic, and migration-inhibitory effects. In vivo, metronomic M344 dosing suppressed tumor growth and extended survival. Combination therapy with M344 and topotecan improved topotecan tolerability, while M344 co-administration with cyclophosphamide reduced tumor rebound post-therapy. In total, M344 demonstrated strong therapeutic potential for NB, offering improved tumor suppression, reduced off-target toxicities, and enhanced control of tumor growth post-therapy. These findings support further investigation of HDAC inhibitors, such as M344, for clinical application in NB treatment.

摘要

神经母细胞瘤(NB)是一种侵袭性儿童癌症,高危患者的五年生存率约为50%。包括手术、化疗、放疗和免疫疗法在内的标准疗法会带来显著的长期毒性且频繁复发。鉴于组蛋白去乙酰化酶(HDAC)抑制剂在调节基因表达和肿瘤表型方面的作用,它们已成为有前景的癌症治疗药物。本研究评估了HDAC抑制剂M344[4-(二甲基氨基)-N-(7-(羟基氨基)-7-氧代庚基)苯甲酰胺]对NB的疗效和作用机制。对临床NB基因表达综合数据库数据的分析显示,晚期肿瘤相对于早期样本表现出更高的HDAC表达。M344治疗有效增加了组蛋白乙酰化,诱导G0/G1期细胞周期停滞,并激活了半胱天冬酶介导的细胞死亡。相对于伏立诺他(一种用于淋巴瘤临床治疗且正在进行NB临床试验的HDAC抑制剂),M344表现出更强的细胞生长抑制、细胞毒性和迁移抑制作用。在体内,节律性给予M344可抑制肿瘤生长并延长生存期。M344与拓扑替康联合治疗提高了拓扑替康的耐受性,而M344与环磷酰胺联合使用可减少治疗后肿瘤的反弹。总体而言,M344对NB显示出强大的治疗潜力,具有更好的肿瘤抑制效果、更低的脱靶毒性以及增强的治疗后肿瘤生长控制能力。这些发现支持进一步研究HDAC抑制剂(如M344)在NB治疗中的临床应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ef6/12429290/654ed366b241/ijms-26-08494-g001.jpg

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