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A platform for high-throughput screening of DNA-encoded catalyst libraries in organic solvents.


ABSTRACT: We have developed a novel high-throughput screening platform for the discovery of small-molecules catalysts for bond-forming reactions. The method employs an in vitro selection for bond-formation using amphiphilic DNA-encoded small molecules charged with reaction substrate, which enables selections to be conducted in a variety of organic or aqueous solvents. Using the amine-catalysed aldol reaction as a catalytic model and high-throughput DNA sequencing as a selection read-out, we demonstrate the 1200-fold enrichment of a known aldol catalyst from a library of 16.7-million uncompetitive library members.

SUBMITTER: Hook KD 

PROVIDER: S-EPMC5637469 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature

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A platform for high-throughput screening of DNA-encoded catalyst libraries in organic solvents.

Hook K Delaney KD   Chambers John T JT   Hili Ryan R  

Chemical science 20170821 10


We have developed a novel high-throughput screening platform for the discovery of small-molecules catalysts for bond-forming reactions. The method employs an <i>in vitro</i> selection for bond-formation using amphiphilic DNA-encoded small molecules charged with reaction substrate, which enables selections to be conducted in a variety of organic or aqueous solvents. Using the amine-catalysed aldol reaction as a catalytic model and high-throughput DNA sequencing as a selection read-out, we demonst  ...[more]

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