Molecular Design, Synthesis, and Evaluation of SNIPER(ER) That Induces Proteasomal Degradation of ERα

  • Keiichiro Okuhira
  • Yosuke Demizu
  • Takayuki Hattori
  • Nobumichi Ohoka
  • Norihito Shibata
  • Masaaki Kurihara
  • Mikihiko Naito
Part of the Methods in Molecular Biology book series (MIMB, volume 1366)

Abstract

Manipulation of protein stability using small molecules has a great potential for both basic research and clinical therapy. Based on our protein knockdown technology, we recently developed a novel small molecule SNIPER(ER) that targets the estrogen receptor alpha (ERα) for degradation via the ubiquitin–proteasome system. This chapter describes the design and synthesis of SNIPER(ER) compounds, and methods for the evaluation of their activity in cellular system.

Key words

Estrogenreceptor SNIPER Proteinknockdown Ubiquitin–proteasome system Cell death 

Notes

Acknowledgement

This study was supported by Grants-in Aid for Scientific Research from the Japan Society for the Promotion of Science (to M.N., K.O., and N.O.) and by Research Fund from Japan Health Sciences Foundation. We are grateful to Cancer Science, Japanese Cancer Association and John Wiley & Sons Ltd. for allowing the reproduction of figures published in [12].

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Copyright information

© Springer Science+Business Media New York 2016

Authors and Affiliations

  • Keiichiro Okuhira
    • 1
  • Yosuke Demizu
    • 2
  • Takayuki Hattori
    • 1
  • Nobumichi Ohoka
    • 1
  • Norihito Shibata
    • 1
  • Masaaki Kurihara
    • 2
  • Mikihiko Naito
    • 1
  1. 1.Division of Biochemistry and Molecular BiologyNational Institute of Health SciencesKamiyoga, Setagaya-ku, TokyoJapan
  2. 2.Division of Organic ChemistryNational Institute of Health SciencesKamiyoga, Setagaya-ku, TokyoJapan

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