title: Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay.
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.
authors.affiliation: School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea.
authors.forename: Dohyun
authors.initials: D
authors.lastname: Son
authors.affiliation: School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea.
authors.forename: Chung Sub
authors.initials: CS
authors.lastname: Kim
authors.affiliation: School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea.
authors.forename: Kang Ro
authors.initials: KR
authors.lastname: Lee
authors.affiliation: School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea. Electronic address: hyunju85@skku.edu.
authors.forename: Hyun-Ju
authors.initials: HJ
authors.lastname: Park
mesh_terms: D005453:Fluorescence; D056572:Histone Deacetylase Inhibitors / Q000494:pharmacology*; D006801:Humans; D011801:Quinic Acid / Q000494:pharmacology*
chemical_list: D056572:Histone Deacetylase Inhibitors; D011801:Quinic Acid
keywords: Epigenetic modulator; Fluorescence-based assay; HDAC inhibitor; Quinic acid derivatives