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Identification of new aryl hydrocarbon receptor (AhR) antagonists using a zebrafish model.
Jeong, Jieun; Kim, Kun-Hee; Kim, Dong-Young; Chandrasekaran, Gopalakrishnan; Kim, Minhee; Pagire, Suvarna H; Dighe, Mahesh; Choi, Eun Young; Bak, Su-Min; Kim, Eun-Young; Shin, Myung-Geun; Choi, Seok-Yong; Ahn, Jin Hee.
Affiliation
  • Jeong J; Department of Chemistry, Gwangju Institute of Science and Technology, Gwangju 61005, Republic of Korea.
  • Kim KH; Department of Biomedical Sciences, Chonnam National University Medical School, Gwangju, Republic of Korea.
  • Kim DY; Department of Biomedical Sciences, University of Ulsan College of Medicine, Seoul, Republic of Korea.
  • Chandrasekaran G; Department of Biomedical Sciences, Chonnam National University Medical School, Gwangju, Republic of Korea.
  • Kim M; Department of Chemistry, Gwangju Institute of Science and Technology, Gwangju 61005, Republic of Korea.
  • Pagire SH; Department of Chemistry, Gwangju Institute of Science and Technology, Gwangju 61005, Republic of Korea.
  • Dighe M; Department of Chemistry, Gwangju Institute of Science and Technology, Gwangju 61005, Republic of Korea.
  • Choi EY; Department of Biomedical Sciences, University of Ulsan College of Medicine, Seoul, Republic of Korea.
  • Bak SM; Department of Life and Nanopharmaceutical Science and Department of Biology, Kyung Hee University, Seoul, Republic of Korea.
  • Kim EY; Department of Life and Nanopharmaceutical Science and Department of Biology, Kyung Hee University, Seoul, Republic of Korea.
  • Shin MG; Department of Laboratory Medicine, Chonnam National University Medical School, Gwangju, Republic of Korea. Electronic address: mgshin@chonnam.ac.kr.
  • Choi SY; Department of Biomedical Sciences, Chonnam National University Medical School, Gwangju, Republic of Korea. Electronic address: zebrafish@chonnam.ac.kr.
  • Ahn JH; Department of Chemistry, Gwangju Institute of Science and Technology, Gwangju 61005, Republic of Korea. Electronic address: jhahn@gist.ac.kr.
Bioorg Med Chem ; 27(19): 115014, 2019 10 01.
Article de En | MEDLINE | ID: mdl-31358358
ABSTRACT
A new series of 1,3-diketone, heterocyclic and α,ß-unsaturated derivatives were synthesized and evaluated for their AhR antagonist activity using zebrafish and mammalian cells. Compounds 1b, 2c, 3b and 5b showed significant AhR antagonist activity in a transgenic zebrafish model. Among them, compound 3b, and 5b were found to have excellent AhR antagonist activity with IC50 of 3.36 nM and 8.3 nM in a luciferase reporter gene assay. In stem cell proliferation assay, compound 5b elicited marked HSC expansion.
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Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Sujet principal: Récepteurs à hydrocarbure aromatique / Protéines de poisson-zèbre / Chalcones / Facteurs de transcription à motif basique hélice-boucle-hélice Type d'étude: Diagnostic_studies / Prognostic_studies Limites: Animals / Humans Langue: En Journal: Bioorg Med Chem Sujet du journal: BIOQUIMICA / QUIMICA Année: 2019 Type de document: Article
Texte intégral
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Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Sujet principal: Récepteurs à hydrocarbure aromatique / Protéines de poisson-zèbre / Chalcones / Facteurs de transcription à motif basique hélice-boucle-hélice Type d'étude: Diagnostic_studies / Prognostic_studies Limites: Animals / Humans Langue: En Journal: Bioorg Med Chem Sujet du journal: BIOQUIMICA / QUIMICA Année: 2019 Type de document: Article