High-content classification of nucleocytoplasmic import or export inhibitors

Yong Jun Kwon, Auguste Genovesio, Nam Youl Kim, Chul Kim Hi Chul Kim, Sungyong Jung, Brigitte David-Watine, Ulf Nehrbass, Neil Emans*

*Corresponding author for this work

Research output: Contribution to journalArticleResearchpeer-review

7 Citations (Scopus)


Transcription factors of the nuclear factor κ B family are the paradigm for signaling dependent nuclear translocation and are ideally suited to analysis through image-based chemical genetic screening. The authors describe combining high-content image analysis with a compound screen to identify compounds affecting either nuclear import or export. Validation in silico and in vitro determined an EC50 for the nuclear export blocker leptomycin B of 2.4 ng/mL (4.4 nM). The method demonstrated high selectivity (Z′ >0.95), speed, and robustness in a screen of a compound collection. It identified the IκB protein kinase inhibitor BAY 11 7082 as an import inhibitor, the p38 mitogen-activated protein (MAP) kinase inhibitor PD98509 as an import enhancer, and phorbol ester as an export inhibitor. The results establish a robust method for identifying compounds regulating nucleocytoplasmic import or export and also implicate MAP kinases in nuclear import of nuclear factor κ B.

Original languageEnglish
Pages (from-to)621-627
Number of pages7
JournalJournal of Biomolecular Screening
Issue number5
Publication statusPublished - Aug 2007
Externally publishedYes


  • Automation
  • High-content screening
  • Image recognition
  • NF-κB
  • Nucleocytoplasmic transport
  • Second messenger-activated kinases
  • Signal transduction


Dive into the research topics of 'High-content classification of nucleocytoplasmic import or export inhibitors'. Together they form a unique fingerprint.

Cite this