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Journal of Biomolecular Screening
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High-Content Classification of Nucleocytoplasmic Import or Export Inhibitors

Yong-Jun Kwon

Institut Pasteur-Korea, Seongbuk-Gu, Seoul, Korea

Auguste Genovesio

Institut Pasteur-Korea, Seongbuk-Gu, Seoul, Korea, Nuclear Cell Biology Group, Institut Pasteur, Paris, France

Nam Youl Kim

Institut Pasteur-Korea, Seongbuk-Gu, Seoul, Korea

Hi Chul Kim

Institut Pasteur-Korea, Seongbuk-Gu, Seoul, Korea

Sungyong Jung

Institut Pasteur-Korea, Seongbuk-Gu, Seoul, Korea

Brigitte David-Watine

Institut Pasteur-Korea, Seongbuk-Gu, Seoul, Korea

Ulf Nehrbass

Institut Pasteur-Korea, Seongbuk-Gu, Seoul, Korea

Neil Emans

Institut Pasteur-Korea, Seongbuk-Gu, Seoul, Korea, emans{at}pasteur.or.kr

Transcription factors of the nuclear factor {kappa} 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 I{kappa}B 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 {kappa} B. (Journal of Biomolecular Screening 2007:621-627)

Key Words: NF-{kappa}B • nucleocytoplasmic transport • signal transduction • second messenger-activated kinases • high-content screening • automation • image recognition

This version was published on August 1, 2007

Journal of Biomolecular Screening, Vol. 12, No. 5, 621-627 (2007)
DOI: 10.1177/1087057107301319
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