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Elucidating drug targets and mechanisms of action by genetic screens in mammalian cells

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Abstract

Phenotypic screening is a powerful approach to discover small molecules with desired effects on biological systems, which can then be developed into therapeutic drugs. The identification of the target and mechanism of action of compounds discovered in phenotypic screens remains a major challenge. This feature article describes the use of genetic tools to reveal drug targets and mechanisms in mammalian cells. Until recently, RNA interference was the method of choice for such studies. Here, we highlight very recent additions to the genetic toolkit in mammalian cells, including CRISPR, CRISPR interference, and CRISPR activation, and illustrate their usefulness for drug target identification.

Graphical abstract: Elucidating drug targets and mechanisms of action by genetic screens in mammalian cells

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Publication details

The article was received on 27 Mar 2017, accepted on 02 May 2017 and first published on 02 May 2017


Article type: Feature Article
DOI: 10.1039/C7CC02349A
Citation: Chem. Commun., 2017, Advance Article
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    Elucidating drug targets and mechanisms of action by genetic screens in mammalian cells

    M. Kampmann, Chem. Commun., 2017, Advance Article , DOI: 10.1039/C7CC02349A

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