Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay

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• 作者：Dohyun Son ; Chung Sub Kim ; Kang Ro Lee ; Hyun-Ju Park ; ^{hyunju85@skku.edu" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Epigenetic modulator ; Fluorescence-based assay ; Quinic acid derivatives ; HDAC inhibitor
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 May 2016
• 年：2016
• 卷：26
• 期：9
• 页码：2365-2369
• 全文大小：1009 K

文摘

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.