Encoded Library Synthesis Using Chemical Ligation and the Discovery of sEH Inhibitors from a 334-Million Member Library.
| Autor: | Litovchick A; X-Chem Pharmaceuticals, 100 Beaver St., Waltham, MA, USA., Dumelin CE; Novartis Pharma AG, Institutes of Biomedical Research, Basel, Switzerland., Habeshian S; X-Chem Pharmaceuticals, 100 Beaver St., Waltham, MA, USA., Gikunju D; X-Chem Pharmaceuticals, 100 Beaver St., Waltham, MA, USA., Guié MA; X-Chem Pharmaceuticals, 100 Beaver St., Waltham, MA, USA., Centrella P; X-Chem Pharmaceuticals, 100 Beaver St., Waltham, MA, USA., Zhang Y; X-Chem Pharmaceuticals, 100 Beaver St., Waltham, MA, USA., Sigel EA; X-Chem Pharmaceuticals, 100 Beaver St., Waltham, MA, USA., Cuozzo JW; X-Chem Pharmaceuticals, 100 Beaver St., Waltham, MA, USA., Keefe AD; X-Chem Pharmaceuticals, 100 Beaver St., Waltham, MA, USA., Clark MA; X-Chem Pharmaceuticals, 100 Beaver St., Waltham, MA, USA. |
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| Jazyk: | angličtina |
| Zdroj: | Scientific reports [Sci Rep] 2015 Jun 10; Vol. 5, pp. 10916. Date of Electronic Publication: 2015 Jun 10. |
| DOI: | 10.1038/srep10916 |
| Abstrakt: | A chemical ligation method for construction of DNA-encoded small-molecule libraries has been developed. Taking advantage of the ability of the Klenow fragment of DNA polymerase to accept templates with triazole linkages in place of phosphodiesters, we have designed a strategy for chemically ligating oligonucleotide tags using cycloaddition chemistry. We have utilized this strategy in the construction and selection of a small molecule library, and successfully identified inhibitors of the enzyme soluble epoxide hydrolase. |
| Databáze: | MEDLINE |
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