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爱与雨下(金币+1): ~! 2011-08-27 10:36:47
爱与雨下(金币+1): ~! 2011-08-27 10:36:56
wgp880924(金币+25, 翻译EPI+1): 感谢 2011-08-27 13:15:28
It has been argued that evolutionary pressure has “prevalidated” natural products, and thus compounds that are structurally similar, to be able to modulate biological systems (1, 6, 8, 44). 天然产物已经得到进化压力的“提前确证”,因此与天然产物在结构上相似的化合物应该能够对生物系统加以调节。However, such methods inevitably generate compound collections with a relatively low degree of overall scaffold diversity and thus chemical space coverage (9), with an emphasis toward known bioactive regions; that is, the compounds generated would be expected to explore areas of chemical space within the boundaries of, or “close to,” those occupied by known bioactive small molecules. 然而,这些方法不可避免地形成一些整体骨架多样性相对低因此化学空间覆盖范围小的化合物集合。也就是说,产生的化合物涉及的化学空间将是或者接近在已知的生物活性小分子所占据的空间的边界之内。Although the biological relevance of compounds from such regions is expected to be high, it is likely that the low-hanging fruit have already been picked as a consequence of decades of focused investigation, principally by pharmaceutical companies (8, 9).尽管从这些区域得到的化合物有望具有高的生物相关性,但很可能数十年来主要由药业公司开展的相关聚集研究所获甚少。
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