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: UNIVERSITY OF HOUSTON
• 依托单位国家: 美国
• 财政年份: 1986
• 资助国家: 美国
• 起止时间: 1986-07-01 至 1989-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3293790
• 关键词: antineoplastic antibiotics; chemical structure function; drug design /synthesis /production; drug metabolism

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.

双环霉素（1）是一种临床上有用的抗生素。 的机理 这种化疗剂的作用知之甚少。 在这 该建议，对药物生物活性的新解释是 提出了 引用证据支持这些途径。 详细 实验提出，以证实这些假设，以及 确定关键步骤的能量。 “分子传感器”的使用是 在这些机械研究中被推广为诊断辅助工具。 知识 哪条途径是双环霉素介导的正确反应途径 这些过程可能为后续的研究提供分子基础。 区域，并允许未来的一般药物设计进行较少的经验 基础 选择一系列生物力学双环霉素类似物， 建议作为抗菌剂评价的潜在候选物。