...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Biochimica et biophysica acta. Molecular basis of disease: BBA >Connexin hemichannel inhibitors with a focus on aminoglycosides
【24h】

Connexin hemichannel inhibitors with a focus on aminoglycosides

机译：Connexin Hemimannel抑制剂，专注于氨基糖苷

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Connexins are membrane proteins involved directly in cell-to-cell communication through the formation of gap-junctional channels. These channels result from the head-to-head docking of two hemichannels, one from each of two adjacent cells. Undocked hemichannels are also present at the plasma membrane where they mediate the efflux of molecules that participate in autocrine and paracrine signaling, but abnormal increase in hemichannel activity can lead to cell damage in disorders such as cardiac infarct, stroke, deafness, cataracts, and skin diseases. For this reason, connexin hemichannels have emerged as a valid therapeutic target. Know small molecule hemichannel inhibitors are not ideal leads for the development of better drugs for clinical use because they are not specific and/or have toxic effects. Newer inhibitors are more selective and include connexin mimetic peptides, anti-connexin antibodies and drugs that reduce connexin expression such as antisense oligonucleotides. Re-purposed drugs and their derivatives are also promising because of the significant experience with their clinical use. Among these, aminoglycoside antibiotics have been identified as inhibitors of connexin hemichannels that do not inhibit gap-junctional channels. In this review, we discuss connexin hemichannels and their inhibitors, with a focus on aminoglycoside antibiotics and derivatives of kanamycin A that inhibit connexin hemichannels, but do not have antibiotic effect.
机译：Connexins是通过形成间隙连接通道直接涉及细胞对细胞连通的膜蛋白。这些通道由两个血管内的头部对接导致两个相邻单元中的每一个。血浆膜也存在于血浆膜的血浆膜中，其中它们介导参与自分泌和旁静脉信号传导的分子的流出，但血管通道活性的异常增加可能导致心脏梗塞，中风，耳聋，白内障和皮肤等疾病中的细胞损伤疾病。因此，Connexin Hemickanns已成为有效的治疗靶标。了解小分子血管笼抑制剂不理想的临床用药的发育，因为它们不是特异性和/或具有毒性作用。更新的抑制剂更具选择性，包​​括Connexin模拟肽，抗Connexin抗体和药物，其减少Connexin表达如反义寡核苷酸。由于临床使用的重大经验，重新用药和它们的衍生物也是有希望的。其中，已经鉴定了氨基糖苷类抗生素作为Connexin血管瘤的抑制剂，其不抑制间隙连接通道。在本综述中，我们讨论Connexin血管箱及其抑制剂，重点关注氨基糖苷抗生素和Kanamycin A的衍生物，抑制Connexin血管瘤，但没有抗生素效应。

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