The Effects of Combinatorial Chemistry and Technologies on Drug Discovery and Biotechnology – a Mini Review

Abstract

The review will focus on the aspects of combinatorial chemistry and technologies that are more relevant in the modern pharmaceutical process. An historical, critical introduction is followed by three chapters, dealing with the use of combinatorial chemistry/high throughput synthesis in medicinal chemistry; the rational design of combinatorial libraries using computer-assisted combinatorial drug design; and the use of combinatorial technologies in biotechnology. The impact of “combinatorial thinking” in drug discovery in general, and in the examples reported in details, is critically discussed. Finally, an expert opinion on current and future trends in combinatorial chemistry and combinatorial technologies is provided.

Keywords

• combinatorial chemistry
• combinatorial technologies
• compound libraries
• computer-assisted combinatorial drug design
• virtual screening
• display libraries
• chemical tools
• chemical biology
• target identification
• fragment-based drug design
• combinatorial proteomics