Protein‐Templated Dynamic Combinatorial Chemistry: Brief Overview and Experimental Protocol. Issue 22 (29th May 2019)

• Record Type: Journal Article
• Authors: Hartman, Alwin M.; Gierse, Robin M.; Hirsch, Anna K. H.
• Is Part Of: European journal of organic chemistry. Issue 22(2019)
• Page Start: 3581
• Page End: 3590
• Publication Date: 2019-05-29
• Subjects: Target‐directed dynamic combinatorial chemistry -- Protein stability -- Hit identification -- Medicinal chemistry -- Biochemical activity; Chemistry, Organic -- Periodicals; Organic compounds -- Synthesis -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1002/ejoc.201900327
• Languages: English
• ISSNs: 1434-193X

Abstract

Abstract : Dynamic combinatorial chemistry (DCC) is a powerful tool to identify bioactive compounds. This efficient technique allows the target to select its own binders and circumvents the need for synthesis and biochemical evaluation of all individual derivatives. An ever‐increasing number of publications report the use of DCC on biologically relevant target proteins. This minireview complements previous reviews by focusing on the experimental protocol and giving detailed examples of essential steps and factors that need to be considered, such as protein stability, buffer composition and cosolvents. Abstract : This minireview focuses on important aspects concerning the practical handling in protein‐templated dynamic combinatorial chemistry (ptDCC). The best biological and chemical conditions should be harmoniously combined in order to successfully apply ptDCC. Moreover, analytical techniques used to determine which compounds are favored are briefly discussed.