Drugs from the Oceans: Marine Natural Products as Leads for Drug Discovery
Drugs from the Oceans: Marine Natural Products as Leads for Drug Discovery
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DOI：
10.2533/chimia.2017.646
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发表时间：
2017-01-01
期刊：
影响因子：
1.2
通讯作者：
Altmann, Karl-Heinz
中科院分区：
文献类型：
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作者：
Altmann, Karl-Heinz
海洋环境中有大量的物种，它们是各种结构多样的生物活性次级代谢物的来源。目前已知的海洋天然产物大约有27'000种，其中8种是7种上市药物的来源，主要用于治疗癌症。大多数这些药物和目前正在进行临床评价的候选药物（不包括抗体-药物缀合物）是未经修饰的天然产物，但合成化学在发现和/或开发所有批准的海洋衍生药物中发挥了核心作用。在过去的十年中，每年有超过1000种新的海洋天然产物被分离出来，但新的和独特的结构还远远没有耗尽。为了充分利用海洋产生的次级代谢产物的结构多样性为药物发现提供的潜力，将需要对它们的不同生物活性以及新发酵技术，合成有机化学和药物化学之间的生产性相互作用进行广泛评估，以确保化合物供应并实现铅优化。
The marine environment harbors a vast number of species that are the source of a wide array of structurally diverse bioactive secondary metabolites. At this point in time, roughly 27'000 marine natural products are known, of which eight are (were) at the origin of seven marketed drugs, mostly for the treatment of cancer. The majority of these drugs and also of drug candidates currently undergoing clinical evaluation (excluding anti-body- drug conjugates) are unmodified natural products, but synthetic chemistry has played a central role in the discovery and/or development of all but one of the approved marine-derived drugs. More than 1000 new marine natural products have been isolated per year over the last decade, but the pool of new and unique structures is far from exhausted. To fully leverage the potential offered by the structural diversity of marine-produced secondary metabolites for drug discovery will require their broad assessment for different bioactivities and the productive interplay between new fermentation technologies, synthetic organic chemistry, and medicinal chemistry, in order to secure compound supply and enable lead optimization.