Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1368624 | Bioorganic & Medicinal Chemistry Letters | 2016 | 5 Pages |
Abstract
A fluorescence-based cellular assay system was established to identify potential epigenetic modulator ligands. This assay method is to detect the de-repression of an EGFP reporter in cancer cells by the treatment of HDAC (histone deacetylase) or DNMT (DNA methyltransferase) inhibitor. Using this system, we conducted a preliminary screening of in-house natural product library containing extracts and pure compounds, and identified several active compounds. Among them, novel quinic acid derivatives were recognized as excellent HDAC inhibitors by both enzymatic and cell-based HDAC assays.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Dohyun Son, Chung Sub Kim, Kang Ro Lee, Hyun-Ju Park,