• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Reviews in medical virology >HIV fusion and its inhibition in antiretroviral therapy.
【24h】

HIV fusion and its inhibition in antiretroviral therapy.

机译：HIV融合及其在抗逆转录病毒疗法中的抑制作用。

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

The end of the twentieth century saw dramatic improvements in the prognosis of HIV infection brought about by the introduction of new agents (the protease inhibitors and the non-nucleoside reverse transcriptase inhibitors) and their use in highly active combinations. However, the durability of these combination treatments is limited by a number of factors including adverse effects and extensive intra-class cross-resistance so that new antiretrovirals acting on alternative targets and having improved systemic tolerability profiles are required. The HIV binding and entry process offers several potential targets for antiviral interaction. These include gp120 binding to CD4 and to chemokine co-receptor molecules as well as the fusion process itself, which involves interactions between two leucine zipper-like 4-3 repeat regions within gp41 known as heptad repeat (HR)1 and HR2. Peptides such as enfuvirtide (formerly DP178 or T-20), that mimic the HR2 region of gp41, inhibit HIV-1 by a mechanism that is thought to involve competitive binding to HR1. This review summarises the clinical development of enfuvirtide, providing an overview of the pharmacokinetic, efficacy and safety data in various patient populations, and also considers the evidence for the key role of genotypic changes in the HR1 region (amino acids 36-45) in determining viral susceptibility to inhibition by enfuvirtide. Copyright 2004 John Wiley & Sons, Ltd.
机译：二十世纪末，由于引入了新的药物（蛋白酶抑制剂和非核苷逆转录酶抑制剂）并将其用于高活性组合，HIV感染的预后得到了显着改善。但是，这些联合治疗的持久性受到许多因素的限制，包括不利影响和广泛的类内交叉耐药性，因此需要新的抗逆转录病毒药物作用于替代靶标并具有改善的系统耐受性。 HIV的结合和进入过程为抗病毒相互作用提供了多个潜在目标。这些包括gp120与CD4和趋化因子共受体分子的结合以及融合过程本身，该过程涉及gp41中两个亮氨酸拉链状4-3重复区域之间的相互作用，这些区域称为七肽重复（HR）1和HR2。像恩夫韦肽这样的肽（以前称为DP178或T-20），模仿gp41的HR2区域，通过一种竞争性结合HR1的机制抑制HIV-1。这篇综述总结了恩夫韦肽的临床发展，概述了各种患者人群的药代动力学，功效和安全性数据，并考虑了HR1区基因型改变（36-45位氨基酸）在确定中的关键作用的证据。病毒对恩夫韦肽抑制的敏感性。版权所有2004 John Wiley＆Sons，Ltd.

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