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Importazole, a Small Molecule Inhibitor of the Transport Receptor importin-β

Importazole, a Small Molecule Inhibitor of the Transport Receptor importin-β

Jonathan F Soderholm, Stephen L Bird, Petr Kalab, Yasaswini Sampathkumar, Keisuke Hasegawa, Michael Uehara-Bingen, Karsten Weis, Rebecca Heald

ACS Chem Biol. 2011 Jul 15;6(7):700-8.

PMID: 21469738

Abstract:

During interphase, the transport receptor importin-β carries cargoes into the nucleus, where RanGTP releases them. A similar mechanism operates in mitosis to generate a gradient of active spindle assembly factors around mitotic chromosomes. Importin-β and RanGTP have been implicated in additional cellular processes, but the precise roles of the Ran/importin-β pathway throughout the cell cycle remain poorly understood. We implemented a FRET-based, high-throughput small molecule screen for compounds that interfere with the interaction between RanGTP and importin-β and identified importazole, a 2,4-diaminoquinazoline. Importazole specifically blocks importin-β-mediated nuclear import both in Xenopus egg extracts and cultured cells, without disrupting transportin-mediated nuclear import or CRM1-mediated nuclear export. When added during mitosis, importazole impairs the release of an importin-β cargo FRET probe and causes both predicted and novel defects in spindle assembly. Together, these results indicate that importazole specifically inhibits the function of importin-β, likely by altering its interaction with RanGTP. Importazole is a valuable tool to evaluate the function of the importin-β/RanGTP pathway at specific stages during the cell cycle.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP662163817	Importazole		662163-81-7	Price

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