Literature DB >> 19716294

The first Hes1 dimer inhibitors from natural products.

Midori A Arai1, Ayako Masada, Toshiyuki Ohtsuka, Ryoichiro Kageyama, Masami Ishibashi.   

Abstract

In the present study, we developed a high-throughput screening system for small molecule-inhibitors of the basic helix-loop-helix (bHLH) transcriptional repressor factor Hes1. Successful dimerization of Hes1 immobilized on a microplate and fluorophore (Cy3)-labelled Hes1 was confirmed. Using this system, several natural products were identified as the first Hes1 dimer inhibitors. Of these, two compounds which were isolated from myxomycetes (true slime molds) inhibited Hes1 from N box-dependent suppression of the gene expression in C3H10T1/2 cells.

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Year:  2009        PMID: 19716294     DOI: 10.1016/j.bmcl.2009.07.146

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 in total

1.  Small-molecule screening yields a compound that inhibits the cancer-associated transcription factor Hes1 via the PHB2 chaperone.

Authors:  Amelie Perron; Yoshihiro Nishikawa; Jun Iwata; Hiromi Shimojo; Junichiro Takaya; Kumiko Kobayashi; Itaru Imayoshi; Naasson M Mbenza; Mihoko Takenoya; Ryoichiro Kageyama; Yuzo Kodama; Motonari Uesugi
Journal:  J Biol Chem       Date:  2018-03-09       Impact factor: 5.157

Review 2.  Hijacking HES1: how tumors co-opt the anti-differentiation strategies of quiescent cells.

Authors:  Liyun Sang; James M Roberts; Hilary A Coller
Journal:  Trends Mol Med       Date:  2009-12-18       Impact factor: 11.951

3.  Identification and targeting of a HES1-YAP1-CDKN1C functional interaction in fusion-negative rhabdomyosarcoma.

Authors:  Alexander R Kovach; Kristianne M Oristian; David G Kirsch; Rex C Bentley; Changde Cheng; Xiang Chen; Po-Han Chen; Jen-Tsan Ashley Chi; Corinne M Linardic
Journal:  Mol Oncol       Date:  2022-08-29       Impact factor: 7.449

4.  The role of dimerisation and nuclear transport in the Hes1 gene regulatory network.

Authors:  Marc Sturrock; Andreas Hellander; Sahar Aldakheel; Linda Petzold; Mark A J Chaplain
Journal:  Bull Math Biol       Date:  2013-05-18       Impact factor: 1.758

Review 5.  Matching the power of high throughput screening to the chemical diversity of natural products.

Authors:  Curtis J Henrich; John A Beutler
Journal:  Nat Prod Rep       Date:  2013-08-08       Impact factor: 13.423

6.  Total synthesis of lindbladione, a Hes1 dimerization inhibitor and neural stem cell activator isolated from Lindbladia tubulina.

Authors:  Midori A Arai; Yuna Makita; Yumi Yamaguchi; Haruka Kawano; Akiko Suganami; Yutaka Tamura; Masami Ishibashi
Journal:  Sci Rep       Date:  2020-12-08       Impact factor: 4.379

7.  Hes1 inhibitor isolated by target protein oriented natural products isolation (TPO-NAPI) of differentiation activators of neural stem cells.

Authors:  Midori A Arai; Naoki Ishikawa; Mitsuha Tanaka; Kenji Uemura; Noriko Sugimitsu; Akiko Suganami; Yutaka Tamura; Takashi Koyano; Thaworn Kowithayakorn; Masami Ishibashi
Journal:  Chem Sci       Date:  2015-12-01       Impact factor: 9.825

  7 in total

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