Abel Ulrich, Koch Corinna, Speitling Michael, Hansske Friedrich G
bioLeads GmbH, Waldhoferstr. 104, Heidelberg, Germany.
Curr Opin Chem Biol. 2002 Aug;6(4):453-8. doi: 10.1016/s1367-5931(02)00338-1.
Natural sources offer a wealth of chemically diverse compounds that have been evolutionary preselected to modulate biochemical pathways. Several industrial and academic groups are accessing this source using advanced technology platforms. Methods have been reported to generate large and diverse natural-product libraries optimised for high-throughput screening and for a fast discovery process. In addition to prefractionated and pure natural-product libraries, parallel synthesis gives access to synthetic, semi-synthetic and natural-product-like libraries. Natural-product chemistry and organic synthesis are powerful tools for optimising natural leads and for generating new diversity from natural scaffolds. The amalgamation of both may be expected to become an important strategy in future drug design.
天然来源提供了大量化学结构多样的化合物,这些化合物经过进化预先筛选,可调节生化途径。一些工业和学术团体正在使用先进的技术平台获取这一来源。已有报道称,利用方法可生成经过优化的大型多样化天然产物库,以用于高通量筛选和快速发现过程。除了预分级和纯天然产物库外,平行合成还可用于获取合成、半合成和天然产物类似物库。天然产物化学和有机合成是优化天然先导化合物以及从天然骨架生成新多样性的有力工具。预计两者的融合将成为未来药物设计的一项重要策略。