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Cellular thermal shift assay information


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]

  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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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...

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Thermal shift assay

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A thermal shift assay (TSA) measures changes in the thermal denaturation temperature and hence stability of a protein under varying conditions such as...

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to as the Mass Spectrometry Cellular Thermal Shift Assay (MS-CETSA). The Drug Affinity Responsive Target Stability assay follows a similar basic assumption...

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Lundbäck T, Nordlund P, Martinez Molina D (September 2014). "The cellular thermal shift assay for evaluating drug target interactions in cells". Nature Protocols...

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if the protein has distinguishable spectroscopic features, or by enzyme assays if the protein has enzymatic activity. Additionally, proteins can be isolated...

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molecules in cells behave in radically different ways than in test-tube assays. Consequently, measurements of the properties of enzymes or processes in...

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antibodies in sensors: 1. The antibody binding capacity is strongly dependent on assay conditions (e.g. pH and temperature), and 2. the antibody-antigen interaction...

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