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烟云听雨铁杆木虫 (正式写手)
金虫
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[求助]
求翻译一段英文文献
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Nature continues to provide a wealth of new leads for potential therapeutic agents or pharmacological probes (1). The role of natural products in traditional medicine is well appreciated and has led to many important drugs that either retain the entire natural product structure or that incorporate (usually straightforward) chemical modifications. Today, biologically useful natural products are most commonly discovered through target-based or phenotypic screening, even in the absence of detailed information about the purpose of the natural product in its original biological setting. The success of these efforts has led some researchers to suggest that scaffolds related to natural product substructures may lead to useful chemical libraries due to the presumed preoptimization of these structures by natural selection (2–4). This argument loses force as compounds become less similar to the natural products that inspired them, but the use of even highly truncated natural product structures in screening can bear fruit if care is taken to retain features consistent with macromolecular binding in the process (5–9). Moreover, it is reasonable to expect that one’s chances for success in identifying structures having activities unrelated to the (possibly unknown) original impetus for evolutionary structure optimization increase if (i) the natural product has multiple bioactivities and (ii) the structure is sufficiently malleable for analogue construction. |
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【答案】应助回帖
★ ★
Mally89(金币+2): 感谢应助!~ 2011-06-03 11:38:47
烟云听雨(金币+10, 翻译EPI+1): 非常感谢 2011-06-03 11:47:41
Mally89(金币+2): 感谢应助!~ 2011-06-03 11:38:47
烟云听雨(金币+10, 翻译EPI+1): 非常感谢 2011-06-03 11:47:41
| 自然界不断为潜在的治疗药物或药理探针提供新的财富(1)。传统医药中的天然成分十分重要,它使得许多重要的药物要么保留完整的天然的产品结构,要么保留合并的(通常是直接的)化学修饰。今天,即使缺乏天然产品在原初的生物过程中的作用的详细信息,人们还是通过基于目标或表型的筛选发现很多生物学上有用的天然产品。这些努力的成功,使一些研究人员认为,根据这些结构存在自然选择的预优化的假设,可以将于天然产物结构相关的基团可以组成有用的化学库(2–4)。如果化合物变得与其原来的前体不是很一致,这种说法就不是很正确了,但是如果小心的保留与大分子结合过程相关的特征结构,即使运用高度截短的天然产物结构进行筛选也能成功(5–9)。此外,如果(i)天然产物有多种生物学活性,(ii)其结构对于类似物的构建具有足够的延展性,则期望在定义结构方面获得成功与增加进化结构选择的最初动力(可能是未知的)无关,这也是合理的。 |

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