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PLANE FACTS ON THE MODE OF ACTION OF BICYCLOMYCIN

PLANE FACTS ON THE MODE OF ACTION OF BICYCLOMYCIN
关于双环霉素作用方式的基本事实
批准号:
3293790
负责人:
HAROLD Lewis KOHN
金额:
$12.03万
依托单位:
依托单位国家:
美国
项目类别:
财政年份:
1986
资助国家:
美国
项目状态:
已结题
起止时间:
1986-07-01 至 1989-06-30

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中文摘要
翻译
双环素(1)是一种临床有用的抗生素。它的作用机制 人们对这种化疗药物的作用知之甚少。在这 提议,对药物的生物活性的一个新的解释是 呈上了。证据被引用来支持这些途径。详细 我们建议用实验来证实这些假说,以及 确定关键步骤的能量值。“分子传感器”的使用是 在这些机械学研究中作为诊断辅助工具被推广。了解以下内容 双环素介导的正确反应途径是什么 这些过程可能为后续的研究提供分子基础。 并允许未来的一般药物设计在经验较少的情况下进行 基础。一系列精选的生物力学双环素类似物是 被认为是抗菌剂评估的潜在候选者。
英文摘要
Bicyclomycin (1) is a clinically useful antibiotic. The mechanism of action of this chemotherapeutic agent is poorly understood. In this proposal, a novel explanation for the biological activity of the drug is presented. Evidence is cited in support of these pathways. Detailed experiments are proposed to substantiate these hypotheses as well as to determine the energetics of key steps. The use of "molecular sensors" is promoted as diagnostic aids in these mechanistic studies. Knowledge of which route is the correct reaction pathway in bicyclomycin mediated processes may provide the molecular basis for subsequent research in this area and allow future general drug design to proceed on a less empirical basis. A select series of biomechanistic bicyclomycin analogues are proposed as potential candidates for antimicrobial evaluation.
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