Department of Medicinal Chemistry, University of Florida, Gainesville, FL 32610, USA.
Future Med Chem. 2011 Sep;3(12):1475-89. doi: 10.4155/fmc.11.118.
The largely unexplored marine world that presumably harbors the most biodiversity may be the vastest resource to discover novel 'validated' structures with novel modes of action that cover biologically relevant chemical space. Several challenges, including the supply problem and target identification, need to be met for successful drug development of these often complex molecules; however, approaches are available to overcome the hurdles. Advances in technologies such as sampling strategies, nanoscale NMR for structure determination, total chemical synthesis, fermentation and biotechnology are all crucial to the success of marine natural products as drug leads. We illustrate the high degree of innovation in the field of marine natural products, which in our view will lead to a new wave of drugs that flow into the market and pharmacies in the future.
可能蕴藏着最多生物多样性的广阔海洋世界在很大程度上尚未被探索,这可能是发现具有新颖作用模式的新型“经过验证”结构的最广阔资源,这些结构涵盖了具有生物学相关性的化学空间。这些通常复杂的分子要成功开发成药物,需要克服包括供应问题和靶点识别在内的多项挑战;然而,有办法可以克服这些障碍。采样策略、用于结构确定的纳米级 NMR、全化学合成、发酵和生物技术等技术的进步对于海洋天然产物作为药物先导物的成功至关重要。我们展示了海洋天然产物领域的高度创新性,我们认为这将导致未来有一波新药涌入市场和药店。