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J Biomol Screen. 2007 Aug;12(5):621-7. Epub 2007 May 16.

High-content classification of nucleocytoplasmic import or export inhibitors.

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


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 EC(50) 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 IkappaB 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.

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