Novel selection methods for DNA-encoded chemical libraries.
Driven by the need for new compounds to serve as biological probes and leads for therapeutic development and the growing accessibility of DNA technologies including high-throughput sequencing, many academic and industrial groups have begun to use DNA-encoded chemical libraries as a source of bioactive small molecules. In this review, we describe the technologies that have enabled the selection of compounds with desired activities from these libraries. These methods exploit the sensitivity of in vitro selection coupled with DNA amplification to overcome some of the limitations and costs associated with conventional screening methods. In addition, we highlight newer techniques with the potential to be applied to the high-throughput evaluation of DNA-encoded chemical libraries.
Department of Chemistry and Chemical Biology and Howard Hughes Medical Institute, Harvard University, 12 Oxford St, Cambridge, MA 02138, United States.
Alix I
AI
Chan
Department of Chemistry and Chemical Biology and Howard Hughes Medical Institute, Harvard University, 12 Oxford St, Cambridge, MA 02138, United States.
Lynn M
LM
McGregor
Department of Chemistry and Chemical Biology and Howard Hughes Medical Institute, Harvard University, 12 Oxford St, Cambridge, MA 02138, United States. Electronic address: drliu@fas.harvard.edu.
David R
DR
Liu
D020650:Combinatorial Chemistry Techniques; D055808:Drug Discovery; D015870:Gene Expression; D015723:Gene Library; D057166:High-Throughput Screening Assays; D006801:Humans; D021141:Nucleic Acid Amplification Techniques; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000378:metabolism
D054852:Small Molecule Libraries