title: A Synthetic Transcriptional Activator of Genes Associated with the Retina in Human Dermal Fibroblasts.
abstract: Small molecules capable of modulating epigenetic signatures can activate the transcription of tissue-restricted genes in a totally unrelated cell type and have potential use in epigenetic therapy. To provide an example for an initial approach, we report here on one synthetic small-molecule compound-termed "SAHA-PIP X"-from our library of conjugates. This compound triggered histone acetylation accompanied by the transcription of retinal-tissue-related genes in human dermal fibroblasts (HDFs).
authors.affiliation: Department of Chemistry, Graduate School of Science Kyoto University, Kitashirakawa-oiwakecho, Sakyo-ku, Kyoto 606-8502 (Japan).
authors.forename: Junetha
authors.initials: J
authors.lastname: Syed
authors.affiliation: Department of Chemistry, Graduate School of Science Kyoto University, Kitashirakawa-oiwakecho, Sakyo-ku, Kyoto 606-8502 (Japan).
authors.forename: Anandhakumar
authors.initials: A
authors.lastname: Chandran
authors.affiliation: Institute for Integrated Cell-Material Sciences (WPI-iCeMS), Kyoto University, Yoshida-ushinomiyacho, Sakyo-ku, Kyoto 606-8501 (Japan).
authors.forename: Ganesh N
authors.initials: GN
authors.lastname: Pandian
authors.affiliation: Department of Chemistry, Graduate School of Science Kyoto University, Kitashirakawa-oiwakecho, Sakyo-ku, Kyoto 606-8502 (Japan).
authors.forename: Junichi
authors.initials: J
authors.lastname: Taniguchi
authors.affiliation: Institute for Integrated Cell-Material Sciences (WPI-iCeMS), Kyoto University, Yoshida-ushinomiyacho, Sakyo-ku, Kyoto 606-8501 (Japan).
authors.forename: Shinsuke
authors.initials: S
authors.lastname: Sato
authors.affiliation: Department of Chemistry, Graduate School of Science Kyoto University, Kitashirakawa-oiwakecho, Sakyo-ku, Kyoto 606-8502 (Japan).
authors.forename: Kaori
authors.initials: K
authors.lastname: Hashiya
authors.affiliation: Department of Chemistry, Graduate School of Science Kyoto University, Kitashirakawa-oiwakecho, Sakyo-ku, Kyoto 606-8502 (Japan).
authors.forename: Gengo
authors.initials: G
authors.lastname: Kashiwazaki
authors.affiliation: Department of Chemistry, Graduate School of Science Kyoto University, Kitashirakawa-oiwakecho, Sakyo-ku, Kyoto 606-8502 (Japan).
authors.forename: Toshikazu
authors.initials: T
authors.lastname: Bando
authors.affiliation: Department of Chemistry, Graduate School of Science Kyoto University, Kitashirakawa-oiwakecho, Sakyo-ku, Kyoto 606-8502 (Japan). hs@kuchem.kyoto-u.ac.jp.|Institute for Integrated Cell-Material Sciences (WPI-iCeMS), Kyoto University, Yoshida-ushinomiyacho, Sakyo-ku, Kyoto 606-8501 (Japan). hs@kuchem.kyoto-u.ac.jp.
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Sugiyama
mesh_terms: D000107:Acetylation / Q000187:drug effects*; D002460:Cell Line; D044127:Epigenesis, Genetic / Q000187:drug effects; D005347:Fibroblasts / Q000187:drug effects* / Q000378:metabolism; D020869:Gene Expression Profiling; D006657:Histones / Q000235:genetics / Q000378:metabolism*; D006801:Humans; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology; D011758:Pyrroles / Q000737:chemistry / Q000494:pharmacology*; D012160:Retina / Q000378:metabolism*; D012164:Retinal Diseases / Q000235:genetics; D054852:Small Molecule Libraries / Q000737:chemistry / Q000494:pharmacology*; D015533:Transcriptional Activation / Q000187:drug effects*
chemical_list: D006657:Histones; D007093:Imidazoles; D011758:Pyrroles; D054852:Small Molecule Libraries
keywords: DNA recognition; artificial transcription activators; gene expression; histone acetylation; transcription profiling