Cellular thermal shift assay

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CEllular Thermal Shift Assay (CETSA®) is a patented label free chemoproteomics 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][4][5]

References

  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. S2CID 5225262.
  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. S2CID 206558838.
  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. PMC 4820820.
  4. ^ "CETSA". CETSA. Retrieved 2021-06-23.
  5. ^ "Alpha CETSA Knowledgebase". PerkinElmer. Retrieved 2021-06-23.


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