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Curr Opin Struct Biol. 2014 Oct;28:105-11. doi: 10.1016/j.sbi.2014.08.007. Epub 2014 Aug 30.

HDX-MS guided drug discovery: small molecules and biopharmaceuticals.

Author information

1
Molecular Therapeutics Department, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, United States.
2
Molecular Therapeutics Department, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, United States. Electronic address: pgriffin@scripps.edu.

Abstract

Hydrogen/deuterium exchange coupled with mass spectrometry (HDX-MS or DXMS) has emerged as an important tool for the development of small molecule therapeutics and biopharmaceuticals. Central to these advances have been improvements to automated HDX-MS platforms and software that allow for the rapid acquisition and processing of experimental data. Correlating the HDX-MS profile of large numbers of ligands with their functional outputs has enabled the development of structure activity relationships (SAR) and delineation of ligand classes based on functional selectivity. HDX-MS has also been applied to address many of the unique challenges posed by the continued emergence of biopharmaceuticals. Here we review the latest applications of HDX-MS to drug discovery, recent advances in technology and software, and provide perspective on future outlook.

PMID:
25179005
PMCID:
PMC4253076
DOI:
10.1016/j.sbi.2014.08.007
[Indexed for MEDLINE]
Free PMC Article

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