Journal
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
Volume 2019, Issue 22, Pages 3581-3590Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201900327
Keywords
Target-directed dynamic combinatorial chemistry; Protein stability; Hit identification; Medicinal chemistry; Biochemical activity
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Funding
- Netherlands Organisation for Scientific Research (VIDI grant) [723.014.008]
- Netherlands Organisation for Scientific Research (LIFT grant) [731.015.414]
- Helmholtz Association's Initiative and Networking Fund
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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.
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