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Marine Natural Products. Key Advances to the Practical Application of this Resource in Drug Development

机译:海洋天然产物。该资源在药物开发中的实际应用的主要进展

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摘要

Over a half century has passed since the first discovery of spongothymidine and spongouridine. These sponge-derived natural products initiated a chain of events that has resulted in countless lives saved from viral infections and cancer. In addition these humble marine products inspired the critical evaluation of marine life for the production of novel chemistry and new drug leads. The resulting natural products chemistry from these efforts is unprecedented in regard to structural complexity and biological activity. The drug leads based on marine natural products have however created unique challenges in scaleable production and structural optimization to evaluate toxicity and enhance biological activity. In this report we have focused our discussion on the progress toward the development of general methodologies for the production, optimization and development of rare but promising marine natural product drug leads. Key developments discussed briefly include sourcing, lead optimization, molecular biology and phylogeny, marine microbial culture, and tools for structure assignment.
机译:自从首次发现海绵体嘧啶和海绵脲以来,已经过去了半个多世纪。这些源自海绵的天然产物引发了一系列事件,导致因病毒感染和癌症而挽救了无数生命。此外,这些不起眼的海洋产品还激发了对海洋生物进行批判性评估以生产新型化学物质和新药物的可能性。这些努力所产生的天然产物化学方面在结构复杂性和生物活性方面是空前的。然而,基于海洋天然产物的药物线索在规模化生产和结构优化以评估毒性和增强生物活性方面提出了独特的挑战。在本报告中,我们集中讨论了开发用于生产,优化和开发稀有但很有前途的海洋天然产物药物线索的一般方法的进展。简要讨论的主要发展包括采购,铅优化,分子生物学和系统发育,海洋微生物培养以及结构分配工具。

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