Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

By D. M. Molina, R. Jafari, M. Ignatushchenko, T. Seki, E. Larsson, Chen Dan, L. Sreekumar, Yihai Cao, Pär Nordlund. 2013

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Tracking cancer drugs in living cells by thermal profiling of the proteome (2014, methodology): “Around their intrinsic melting temperature, proteins in the cell denature and subsequently aggregate (16), resulting in their gradual disappearance from the PBS-extracted samples with increasing temperatures (12, 17).”
Natural Products for Drug Discovery in the 21st Century: Innovations for Novel Drug Discovery (2018, methodology): “This method has been useful in identifying target proteins of many anti-cancer therapeutic agents such as raltitrexed and methotrexate [145].”
Target identification with quantitative activity based protein profiling (ABPP) (2017, methodology): “…methods including the previously mentioned AfBPP approach as well as novel protein stability focused approaches such as drug afﬁnity responsive target stability [15,16] and the cellular thermal shift assay [98,99], which are based on biophysical principles of ligand-induced protein stabilization.”