Schneider Gisbert, Fechner Uli
Johann Wolfgang Goethe-University, Institute of Organic Chemistry and Chemical Biology, Marie-Curie-Str. 11 D-60439 Frankfurt am Main, Germany.
Nat Rev Drug Discov. 2005 Aug;4(8):649-63. doi: 10.1038/nrd1799.
Ever since the first automated de novo design techniques were conceived only 15 years ago, the computer-based design of hit and lead structure candidates has emerged as a complementary approach to high-throughput screening. Although many challenges remain, de novo design supports drug discovery projects by generating novel pharmaceutically active agents with desired properties in a cost- and time-efficient manner. In this review, we outline the various design concepts and highlight current developments in computer-based de novo design.
自15年前首次构思出第一代自动化从头设计技术以来,基于计算机的苗头化合物和先导化合物结构候选物设计已成为高通量筛选的一种补充方法。尽管仍存在许多挑战,但从头设计通过以具有成本效益和时间效益的方式生成具有所需特性的新型药物活性剂,为药物发现项目提供了支持。在本综述中,我们概述了各种设计概念,并突出了基于计算机的从头设计的当前进展。