Interrogating fragments using a protein thermal shift assay

McMahon, Róisín M., Scanlon, Martin J. and Martin, Jennifer L. (2013) Interrogating fragments using a protein thermal shift assay. Australian Journal of Chemistry, 66 12: 1502-1506. doi:10.1071/CH13279

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Author McMahon, Róisín M.
Scanlon, Martin J.
Martin, Jennifer L.
Title Interrogating fragments using a protein thermal shift assay
Journal name Australian Journal of Chemistry   Check publisher's open access policy
ISSN 0004-9425
Publication date 2013-09-05
Sub-type Critical review of research, literature review, critical commentary
DOI 10.1071/CH13279
Open Access Status File (Author Post-print)
Volume 66
Issue 12
Start page 1502
End page 1506
Total pages 5
Place of publication Collingwood, VIC, Australia
Publisher C S I R O Publishing
Language eng
Formatted abstract
Protein thermal shift is a relatively rapid and inexpensive technique for the identification of low molecular weight compound interactions with protein targets. An increase in the melting temperature of the target protein in the presence of a test ligand is indicative of a promising ligand–protein interaction. Due to its simplicity, protein thermal shift is an attractive method for screening libraries and validating hits in drug discovery programs. The methodology has been used successfully in high throughput screens of small molecule libraries, and its application has been extended to report on protein–drug-like-fragment interactions. Here, we review how protein thermal shift has been employed recently in fragment-based drug discovery (FBDD) efforts, and highlight its application to protein–protein interaction targets. Multiple validation of fragment hits by independent means is paramount to ensure efficient and economical progress in a FBDD campaign. We discuss the applicability of thermal shift assays in this light, and discuss more generally what one does when orthogonal approaches disagree.
Keyword Thermal shift assays
Fragment based drug discovery
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Critical review of research, literature review, critical commentary
Collections: Official 2014 Collection
Institute for Molecular Bioscience - Publications
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Citation counts: TR Web of Science Citation Count  Cited 2 times in Thomson Reuters Web of Science Article | Citations
Scopus Citation Count Cited 5 times in Scopus Article | Citations
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Created: Tue, 24 Dec 2013, 18:50:02 EST by Roisin Mcmahon on behalf of Chemistry, Department of