文摘

利用纳米生物寻找新药的发现

作者(年代):彼得·卢卡斯

虽然“rule-of-five”(也称为“利平斯基的drug-likeness规则”)是一个非常有用的指导设计口头访问小分子药物,它在某些方面被过分夸大。首先,只有51%的小分子药物得到FDA的批准是口服,坚持“rule-of-five。”This doesn't even take into account the growing number of biologicals, some of which have become "blockbuster" hits. Secondly, it does not encompass natural product and semisynthetic natural product medications, which constitute roughly one-third of all marketed small-molecule pharmaceuticals. Instead of relying too heavily on 'rule-of-five' compliance, a more balanced and systematic approach to药物发现应该更加丰硕。这些尤其重要,当试图打击“一流”和/或极其困难的目标,这种蛋白酶和那些涉及蛋白质-蛋白质之间的关系。此外,更大的工作应该进入研究天然产物。合成生物学,包括基因改变生物小分子药物,可以解决一些困难的问题基于产品天然药物开发,如合成配体的效率和可行性。