Single dish gradient screening of small molecule localization

Understanding trafficking in cells and tissues is one of the most critical steps in exploring the mechanisms and modes of action (MOAs) of a small molecule. Typically, deciphering the role of concentration presents one of the most difficult challenges associated with this task. Herein, we present a...

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Bibliographic Details
Published in:Organic & biomolecular chemistry 2016-09, Vol.14 (35), p.8241-8245
Main Authors: Beuzer, Paolo, Axelrod, Joshua, Trzoss, Lynnie, Fenical, Willam, Dasari, Ramesh, Evidente, Antonio, Kornienko, Alexander, Cang, Hu, La Clair, James J
Format: Article
Language:English
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Summary:Understanding trafficking in cells and tissues is one of the most critical steps in exploring the mechanisms and modes of action (MOAs) of a small molecule. Typically, deciphering the role of concentration presents one of the most difficult challenges associated with this task. Herein, we present a practical solution to this problem by developing concentration gradients within single dishes of cells. We demonstrate the method by evaluating fluorescently-labelled probes developed from two classes of natural products that have been identified as potential anti-cancer leads by STORM super-resolution microscopy. Understanding trafficking in cells and tissues is one of the most critical steps in exploring the mechanisms and modes of action (MOAs) of a small molecule.
ISSN:1477-0520
1477-0539
DOI:10.1039/c6ob01418f