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Issue 63, 2019
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Target engagement approaches for pharmacological evaluation in animal models

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Abstract

The field of chemical biology has introduced several approaches, typically using chemical probes, to measure the direct binding interaction of a small molecule with its biological target in cells. The use of these direct target engagement assays in pharmaceutical development can support mechanism of action hypothesis testing, rank ordering of compounds, and iterative improvements of chemical matter. This Feature Article highlights a newer application of these approaches: the quantification of target engagement in animal models to support late stage preclinical development and the nomination of a drug candidate to clinical trials. Broadly speaking, these efforts can be divided between compounds that covalently and reversibly interact with protein targets; recent examples for both categories are discussed for a range of targets, along with their limitations. New, promising technologies are also highlighted, in addition to the application of target engagement determination to new therapeutic modalities.

Graphical abstract: Target engagement approaches for pharmacological evaluation in animal models

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Article information


Submitted
11 Apr 2019
Accepted
11 Jul 2019
First published
22 Jul 2019

Chem. Commun., 2019,55, 9241-9250
Article type
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Target engagement approaches for pharmacological evaluation in animal models

J. E. Kath and A. Baranczak, Chem. Commun., 2019, 55, 9241
DOI: 10.1039/C9CC02824B

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