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Drug discovery goes cm naturel

机译:药物发现走向自然

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Discovering useful drugs to treat tuberculosis is not an exercise for the faint of heart. Screening for agents that inhibit the growth of the causative mycobacterium produces very few hits, and optimizing those hits into drug-like 'lead' molecules is exceptionally difficult, owing to the bacterium's impermeable cell envelope. Even armed with a promising lead, animal models and early-stage clinical trials have little predictive value, and the long duration of therapy currently required to treat tuberculosis makes safety hurdles much higher than for most bacterial infections. So, an attractive strategy, and one that lies at the heart of a report by Lee et al. in Nature Medicine, is to repurpose an existing antibiotic class that is already known to be safe and effective in other infections, but that has poor antitubercular activity.
机译:寻找有用的药物来治疗肺结核并不是轻率的事情。筛选抑制致病性分枝杆菌生长的药物产生的命中极少,由于细菌的不可渗透细胞包膜,将这些命中优化为药物样“前导”分子非常困难。即使拥有有前途的领导者,动物模型和早期临床试验也没有什么预测价值,而且目前治疗结核病所需的长期治疗使安全性障碍远远超过大多数细菌感染。因此,这是一种有吸引力的策略,而这正是Lee等人的报告的核心。 Nature Medicine的研究人员是将现有的抗生素类别重新利用,该类别在其他感染中是安全有效的,但抗结核活性差。

著录项

  • 来源
    《Nature》 |2014年第7489期|436-437|共2页
  • 作者

    CLIFTON E. BARRY;

  • 作者单位

    Tuberculosis Research Section, National Institute of Allergy and Infectious Diseases, Bethesda, Maryland 20892-3206, USA;

  • 收录信息 美国《科学引文索引》(SCI);美国《工程索引》(EI);美国《生物学医学文摘》(MEDLINE);美国《化学文摘》(CA);
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

  • 入库时间 2022-08-18 02:52:57

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