Development of the artificial transcription factor which promotes endogenous gene expression in cell

2011 Fiscal Year Final Research Report

• Project/Area Number: 22750151
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Single-year Grants
• Research Field: Chemistry related to living body
• Research Institution: Kyoto University
• Principal Investigator: SHIMOGAWA Hiroki 京都大学, 化学研究所, 助教 (70447928)
• Project Period (FY): 2010 – 2011
• Keywords: レンチノロール / 転写因子 / 転写活性化 / 小分子有機化合物 / 細胞膜透過性 / Sur2 / アダマンタン

Research Abstract

The wrenchnolol analogue was developed, it has improved water solubility and with lower molecule weight.
The compound 10 which reported have transcriptional activation ability was synthesized, and this compound was assayed by transcriptional activation assay using streptavidin-biotin system. As the result, by this system, the compound 10 did not show transcriptional activation ability.
The transcriptional activation ability of the compound 10 was measured using glucocorticoid receptor-dexamethasone system. By this system, the compound 10 also did not show transcriptional activation ability.

Research Products

• [Journal Article] Synthesis and Evaluation of Diaryl Thiazole Derivatives that Inhibit Activation of Sterol Regulatory Element-Binding Proteins (2011)
  • Author(s): Kamisuki, S.; Shirakawa, T.; Kugimiya A.; Abu-Elheiga, L.; Choo, P. H.; Yamada, K.; Shimogawa, H.; Wakil, J. S.; Uesugi, M
  • Journal Title: Journal of Medicinal Chemistry Volume: 54 Pages: 4923-4927
  • DOI: DOI:10.1021/jm200304y
  • Peer Reviewed
• [Journal Article] A Mitochondrial Surface-Specific Fluorescent Probe Activated by Bioconversion (2011)
  • Author(s): Kawazoe Y.; Shimogawa, H.; Sato, A.; Uesugi, M. Angew
  • Journal Title: Chem. Int. Ed Volume: 50 Pages: 5478-5481
  • DOI: DOI:10.1002/anie.201100935
  • Peer Reviewed
• [Journal Article] Cell-Morphology Profiling of a Natural Product Library Identifies Bisebromoamide and Miuraenamide A as Actin Filament Stabilizers (2011)
  • Author(s): Sumiya, E.; Shimogawa, H.; Sasaki, H.; Tsutsumi, M.; Yoshita, K.; Ojika, M.; Suenaga, K.; Uesugi, M
  • Journal Title: ACS Chem. Biol Volume: 6 Pages: 425-431
  • DOI: DOI:10.1021/cb1003459
  • Peer Reviewed
• [Journal Article] Chemical Library Screening Identifies a Small Molecule That Downregulates SOD1 Transcription for Drugs to Treat Amyotrophic Lateral Sclerosis (2011)
  • Author(s): Murakami, G.; Inoue, H.; Tsukita, K.; Asai, Y.; Amagai, Y.; Aiba, K.; Shimogawa, H.; Uesugi, M.; Nakatsuji, N.; Takahashi, R
  • Journal Title: Journal of Biomolecular Screening Volume: 16 Pages: 405-414
  • DOI: DOI:10.1177/1087057110397888
  • Peer Reviewed
• [Presentation] Morphology-based screening for the identification of actin-interfering compounds (2010)
  • Author(s): Eriko Sumiya, Hiroki Shimogawa, Hiroaki Sasaki, Makoto Ojika, Kiyotake Suenaga, Motonari Uesugi
  • Organizer: PACIFICHEM2010
  • Place of Presentation: Hawaii Hawaii convention center
  • Year and Date: 2010-12-15
• [Presentation] 細胞形態変化誘導活性を指標としたアクチン阻害化合物の探索 (2010)
  • Author(s): 住谷瑛理子・下川浩輝・佐々木宏明・小鹿一・末永聖武・上杉志成
  • Organizer: 第29回メディシナルケミストリーシンポジウム
  • Place of Presentation: 京都京都テルサ
  • Year and Date: 2010-11-17
• [Presentation] 細胞形態変化誘導活性を指標としたアクチン阻害化合物の探索 (2010)
  • Author(s): 住谷瑛理子・下川浩輝・佐々木宏明・小鹿一・末永聖武・上杉志成
  • Organizer: 第52回天然有機化合物討論会
  • Place of Presentation: 静岡静岡県コンベンションアーツセンター
  • Year and Date: 2010-09-29
• [Presentation] 海洋天然物Bisebromoamideによるアクチン線維の安定化 (2010)
  • Author(s): 住谷瑛理子・下川浩輝・佐々木宏明・末永聖武・上杉志成
  • Organizer: 日本ケミカルバイオロジー学会第5回年会
  • Place of Presentation: 横浜慶応義塾大学
  • Year and Date: 2010-05-18
• [Presentation] 転写を制御する小分子有機化合物 (2010)
  • Author(s): 下川浩輝
  • Organizer: 第130年会日本薬学会
  • Place of Presentation: 岡山岡山大学
  • Year and Date: 2010-03-28
• [Book] ファルマシア第23回化合物推理ゲーム (2010)
  • Author(s): 下川浩輝, 上杉志成
  • Total Pages: 179-182