Cellular thermal shift assay

CEllular Thermal Shift Assay (CETSA) is a patented label free method that has enabled measurements of compound target engagement in intact cells and tissue, without modifications to the target protein. This is accomplished by comparing the measured cellular thermal stability of the protein in the presence and absence of the test compound. An efficacious compound binding to its intended target will affect associated proteins and thereby leave traces in the cell in form of changed signalling patterns. Such patterns can arise from for example loss or gain of protein-protein interactions, phosphorylations or release of regulatory molecules.[1][2][3]

References

Molina, Daniel Martinez; Jafari, Rozbeh; Ignatushchenko, Marina; Seki, Takahiro; Larsson, E. Andreas; Dan, Chen; Sreekumar, Lekshmy; Cao, Yihai; Nordlund, Pär (2013-07-05). "Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay". Science. 341 (6141): 84–87. doi:10.1126/science.1233606. ISSN 0036-8075. PMID 23828940.
Savitski, Mikhail M.; Reinhard, Friedrich B. M.; Franken, Holger; Werner, Thilo; Savitski, Maria Fälth; Eberhard, Dirk; Molina, Daniel Martinez; Jafari, Rozbeh; Dovega, Rebecca Bakszt; Klaeger, Susan; Kuster, Bernhard (2014-10-03). "Tracking cancer drugs in living cells by thermal profiling of the proteome". Science. 346 (6205). doi:10.1126/science.1255784. hdl:10616/42298. ISSN 0036-8075. PMID 25278616.
Almqvist, Helena; Axelsson, Hanna; Jafari, Rozbeh; Dan, Chen; Mateus, André; Haraldsson, Martin; Larsson, Andreas; Molina, Daniel Martinez; Artursson, Per; Lundbäck, Thomas; Nordlund, Pär (2016-03-24). "CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil". Nature Communications. 7 (1): 1–11. doi:10.1038/ncomms11040. ISSN 2041-1723.

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[1] Molina, Daniel Martinez; Jafari, Rozbeh; Ignatushchenko, Marina; Seki, Takahiro; Larsson, E. Andreas; Dan, Chen; Sreekumar, Lekshmy; Cao, Yihai; Nordlund, Pär (2013-07-05). "Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay". Science. 341 (6141): 84–87. doi:10.1126/science.1233606. ISSN 0036-8075. PMID 23828940.

[2] Savitski, Mikhail M.; Reinhard, Friedrich B. M.; Franken, Holger; Werner, Thilo; Savitski, Maria Fälth; Eberhard, Dirk; Molina, Daniel Martinez; Jafari, Rozbeh; Dovega, Rebecca Bakszt; Klaeger, Susan; Kuster, Bernhard (2014-10-03). "Tracking cancer drugs in living cells by thermal profiling of the proteome". Science. 346 (6205). doi:10.1126/science.1255784. hdl:10616/42298. ISSN 0036-8075. PMID 25278616.

[3] Almqvist, Helena; Axelsson, Hanna; Jafari, Rozbeh; Dan, Chen; Mateus, André; Haraldsson, Martin; Larsson, Andreas; Molina, Daniel Martinez; Artursson, Per; Lundbäck, Thomas; Nordlund, Pär (2016-03-24). "CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil". Nature Communications. 7 (1): 1–11. doi:10.1038/ncomms11040. ISSN 2041-1723.