Lead Generation for Challenging Targets

Jinqiao Wan, Dengfeng Dou, Hongmei Song, Xian-Hui Wu, Xuemin Cheng, and Jin U 

Lead Generation Methods, Strate es, and Case Studies, First Edition. Edited by Jorg Holenz. 

DNA sequencing machines. In addition, compared to HTS, DEL demonstrates significant advantages in compound storage and cost-effectiveness. 

Although target-based methods have their limitations, they still demonstrate great potential in rationally designing new molecular entities especially for new target classes, such as PPIs. A famous example is the stapled peptide technology, which mimics a-helical structures in the PPL Short peptides can be stabilized into a-helical structures with the use of various chemical methods. These structures are almost identical to the natural folding and thus interfere with the PPI [9]. 

In this chapter, we give a brief survey of several advanced technologies in lead generation, which demonstrate capabilities for challenging targets. 

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