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ACS Chem Biol. 2018 Feb 16;13(2):366-375. doi: 10.1021/acschembio.7b00965. Epub 2018 Jan 25.

CRISPR Approaches to Small Molecule Target Identification.

Author information

1
Department of Cellular and Molecular Pharmacology, Howard Hughes Medical Institute, Center for RNA Systems Biology, University of California, San Francisco , San Francisco, California 94158, United States.
2
Department of Microbiology and Immunology, University of California, San Francisco , San Francisco, California 94158, United States.

Abstract

A long-standing challenge in drug development is the identification of the mechanisms of action of small molecules with therapeutic potential. A number of methods have been developed to address this challenge, each with inherent strengths and limitations. We here provide a brief review of these methods with a focus on chemical-genetic methods that are based on systematically profiling the effects of genetic perturbations on drug sensitivity. In particular, application of these methods to mammalian systems has been facilitated by the recent advent of CRISPR-based approaches, which enable one to readily repress, induce, or delete a given gene and determine the resulting effects on drug sensitivity.

PMID:
29261286
PMCID:
PMC5834945
DOI:
10.1021/acschembio.7b00965
[Indexed for MEDLINE]
Free PMC Article

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