摘要
组蛋白去乙酰化酶抑制剂(Hdaci)已被证明是一类新兴的抗癌药物,参与调控基因表达和染色质重塑,从而显示出有效的靶点。针对不同类型的癌症治疗。泛去乙酰化酶抑制剂panobinostat(Farydacr,lbh589)是由诺华制药公司和美国食品及药物管理局批准的一种新药物开发的。洛马。它正在进行临床调查的一系列血液学和实体肿瘤世界各地的口服和静脉制剂。泛比诺他汀通过与肿瘤细胞的相互作用抑制肿瘤细胞的生长组蛋白和非组蛋白的乙酰化以及各种凋亡、自噬介导的靶点和各种肿瘤发生途径参与癌症的发展。目前的文章分析了泛比诺体在胃肠道肿瘤中的作用。临床和临床资料表明,帕诺比诺特对肝细胞、胰腺、结直肠、g具有潜在的抑制作用。胃和胃肠道间质瘤。帕诺比诺特的临床评估目前正在进行中。在此,我们还回顾了综合疗法在试验中的基本原理,以及胃肠道肿瘤治疗的前景。
关键词: HDAC,HDACi,Panobinostat,联合治疗,胃肠道肿瘤,临床前和临床研究。
Current Cancer Drug Targets
Title:The Safety, Efficacy and Therapeutic Potential of Histone Deacetylase Inhibitors with Special Reference to Panobinostat in Gastrointestinal Tumors: A Review of Preclinical and Clinical Studies
Volume: 18 Issue: 8
关键词: HDAC,HDACi,Panobinostat,联合治疗,胃肠道肿瘤,临床前和临床研究。
摘要: Histone deacetylase inhibitors (HDACi) have been demonstrated as an emerging class of anticancer drugs involved in regulation of gene expression and chromatin remodeling thus indicating valid targets for different types of cancer therapeutics. The pan-deacetylase inhibitor panobinostat (Farydac®, LBH589) is developed by Novartis Pharmaceuticals and a newly US FDA approved drug for the multiple myeloma. It is under clinical investigation for a range of hematological and solid tumors worldwide in both oral and intravenous formulations. Panobinostat inhibits tumor cell growth by interacting with acetylation of histones and nonhistone proteins as well as various apoptotic, autophagy-mediated targets and various tumorigenesis pathways involved in the development of cancer. The current article summarizes the status of panobinostat in gastrointestinal cancers. Preclinical and clinical data suggest that panobinostat has potential inhibitory activity in hepatocellular, pancreatic, colorectal, gastric and gastrointestinal stromal tumors. Clinical evaluations of panobinostat are currently underway. Herein, we have also reviewed the rationale behind the combination therapy under the trials and possible future prospective for the treatment of GI tumors.
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Cite this article as:
The Safety, Efficacy and Therapeutic Potential of Histone Deacetylase Inhibitors with Special Reference to Panobinostat in Gastrointestinal Tumors: A Review of Preclinical and Clinical Studies, Current Cancer Drug Targets 2018; 18 (8) . https://dx.doi.org/10.2174/1568009617666170630124643
DOI https://dx.doi.org/10.2174/1568009617666170630124643 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
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