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  • 标题:Development of Photoswitchable Estrogen Receptor Ligands
  • 本地全文:下载
  • 作者:Keisuke Tsuchiya ; Tomohiro Umeno ; Genichiro Tsuji
  • 期刊名称:Chemical and Pharmaceutical Bulletin
  • 印刷版ISSN:0009-2363
  • 电子版ISSN:1347-5223
  • 出版年度:2020
  • 卷号:68
  • 期号:4
  • 页码:398-402
  • DOI:10.1248/cpb.c19-01108
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Photopharmacology has attracted attention as an approach for the development of novel therapeutics because it allows regulation of the bioactivity of compounds based on their conformational change by photo-irradiation. Previously, we have reported several types of selective estrogen receptor (ER) modulators based on diphenylmethane skeleton. To develop novel photopharmacological reagents, we designed and synthesized a set of ER ligands based on azobenzene skeleton, which can switch its conformation following UV irradiation. Our results showed that after UV irradiation, the Z -form of the synthesized compound 9 interacted with ERα, with a K D value of 2.5 µM, whereas the E -form of compound 9 did not bind ability to ERα at 10 µM..
  • 关键词:estrogen receptor;photopharmacology;diazo moiety;fluorescent polarization assay
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