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Veale et al ChemRxiv 0610.pdf (1.72 MB)
A New Native Mass Spectrometry Platform Identifies Inhibitors of the HSP90 – HOP Protein-Protein Interaction
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submitted on 10.06.2020 and posted on 11.06.2020by Clinton Veale, Mateos-Jimenez, Maria, Michaelone Vaaltyn, Ronel Müller, Matodzi Makhubu, Mahama Alhassan, Beatriz G. de la
Torre, Fernando Albericio, C. Logan Mackay, Adrienne L. Edkins, David Clarke
This communication discusses for the first time, the use of mass spectrometry as a platform for screening for PPI inhibitors, without protein tethering or labeling. Furthermore, in the context of cancer drug discovery, this study demonstrates the ligandability and therefore the potential druggability of HOP, whose PPI with HSP90 has been routinely discussed as a difficult to drug target of substantial potential.