DNA-encoded chemical libraries: foundations and applications in lead discovery
نویسندگان
چکیده
منابع مشابه
DNA-encoded chemical libraries.
The discovery and development of novel drugs for the multitude of targets originating from functional genomic research is a challenging task. While antibodies can nowadays be raised against virtually any given target using phage-display methodologies, a similar "selection/amplification" approach for the facile discovery of low-molecular weight compounds capable of specific binding to protein ta...
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Discovery of small molecule inhibitors of protein-protein interactions (PPIs) has been limited due to technological hurdles. Here we present the discovery of small molecule (MW< 500 Da) inhibitors of PPIs with IC50 in the μM range from a 2 million compound DNA-encoded chemical library. The screening of the library was performed using a recently developed homogenous binding assay. This format av...
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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 ...
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A method for the encoding of split/mix combinatorial chemical libraries based on Euclidean shapes is described. The shapes are fashioned from a polymeric matrix designed to swell in common organic solvents while retaining their unique forms, and exhibit good mechanical strength. The lightly crosslinked gel-type polymer was processed into an array of Euclidean forms that serve as encoding elemen...
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Several drug discovery and design endevours are focused on an exhaustive exploration of the drug-like chemical space with the final goal of identifying compounds that can be developed clinically. The traditional drug-like chemical space has been defined using old drugs with empirical rules such as the Lipinski’s Rule-of-Five (RO5). Therefore, promising drug candidates may be overlooked because ...
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ژورنال
عنوان ژورنال: Drug Discovery Today
سال: 2016
ISSN: 1359-6446
DOI: 10.1016/j.drudis.2016.07.013