• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>BioResearch open access. >Butyrate Histone Deacetylase Inhibitors
【24h】

Butyrate Histone Deacetylase Inhibitors

机译：丁酸酯组蛋白脱乙酰基酶抑制剂

获取原文
       
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

In addition to being a part of the metabolic fatty acid fuel cycle, butyrate is also capable of inducing growth arrest in a variety of normal cell types and senescence-like phenotypes in gynecological cancer cells, inhibiting DNA synthesis and cell growth in colonic tumor cell lines, suppressing hTERT mRNA expression and telomerase activity in human prostate cancer cells, and inducing stem cell differentiation and apoptosis by DNA fragmentation. It regulates gene expression by inhibiting histone deacetylases (HDACs), enhances memory recovery and formation in mice, stimulates neurogenesis in the ischemic brain, promotes osteoblast formation, selectively blocks cell replication in transformed cells (compared to healthy cells), and can prevent and treat diet-induced obesity and insulin resistance in mouse models of obesity, as well as stimulate fetal hemoglobin expression in individuals with hematologic diseases such as the thalassemias and sickle-cell disease, in addition to a multitude of other biochemical effects in vivo . However, efforts to exploit the potential of butyrate in the clinical treatment of cancer and other medical disorders are thwarted by its poor pharmacological properties (short half-life and first-pass hepatic clearance) and the multigram doses needed to achieve therapeutic concentrations in vivo . Herein, we review some of the methods used to overcome these difficulties with an emphasis on HDAC inhibition.
机译：丁酸除了是代谢脂肪酸燃料循环的一部分外，还能够在妇科癌细胞中的多种正常细胞类型和衰老样表型中诱导生长停滞，抑制结肠肿瘤细胞系中的DNA合成和细胞生长。 ，抑制人类前列腺癌细胞中hTERT mRNA表达和端粒酶活性，并通过DNA片段化诱导干细胞分化和凋亡。它通过抑制组蛋白脱乙酰基酶（HDAC）调节基因表达，增强小鼠的记忆恢复和形成，刺激缺血性脑中的神经发生，促进成骨细胞形成，选择性地阻止转化细胞（与健康细胞相比）中的细胞复制，并可以预防和治疗饮食诱发的肥胖症和小鼠肥胖症模型中的胰岛素抵抗，以及血液系统疾病如地中海贫血和镰状细胞病患者的胎儿血红蛋白表达，以及多种其他体内生物化学作用。但是，由于丁酸药理学性能较差（半衰期短和肝首过清除率短）和达到体内治疗浓度所需的毫克剂量，阻碍了在癌症和其他医学疾病的临床治疗中开发丁酸酯潜力的努力。本文中，我们回顾了一些克服这些困难的方法，重点是抑制HDAC。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号