Tri-Institutional Training Program in Chemical Biology, Memorial Sloan-Kettering Cancer Center, 1275 York Ave, Box 422, New York, NY 10065, USA.
Curr Opin Chem Biol. 2010 Jun;14(3):308-14. doi: 10.1016/j.cbpa.2010.02.001. Epub 2010 Mar 2.
Existing drugs address a relatively narrow range of biological targets. As a result, libraries of drug-like molecules have proven ineffective against a variety of challenging targets, such as protein-protein interactions, nucleic acid complexes, and antibacterial modalities. In contrast, natural products are known to be effective at modulating such targets, and new libraries are being developed based on underrepresented scaffolds and regions of chemical space associated with natural products. This has led to several recent successes in identifying new chemical probes that address these challenging targets.
现有的药物针对的是相对较窄的生物靶点范围。因此,类似药物的分子库已被证明对各种具有挑战性的靶点(如蛋白质-蛋白质相互作用、核酸复合物和抗菌模式)无效。相比之下,天然产物在调节这些靶点方面已被证实是有效的,并且正在基于代表性不足的支架和与天然产物相关的化学空间区域来开发新的分子库。这导致了最近在识别针对这些具有挑战性的靶点的新化学探针方面取得了一些成功。