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J Am Chem Soc. 2011 Jan 12;133(1):12-4. doi: 10.1021/ja108258d. Epub 2010 Dec 13.

A photocleavable rapamycin conjugate for spatiotemporal control of small GTPase activity.

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  • 1Department of Cell Biology, Center for Cell Dynamics, Johns Hopkins University, Baltimore, Maryland 21205, USA.


We developed a novel method to spatiotemporally control the activity of signaling molecules. A newly synthesized photocaged rapamycin derivative induced rapid dimerization of FKBP (FK-506 binding protein) and FRB (FKBP-rapamycin binding protein) upon UV irradiation. With this system and the spatially confined UV irradiation, we achieved subcellularly localized activation of Rac, a member of small GTPases. Our technique offers a powerful approach to studies of dynamic intracellular signaling events.

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