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The evolution and application progress of non-modified drug target discovery CETSA technology
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Guang-yuan LIU, Ya-hui LI, Wei ZHANG*, De-zhi KONG*
Acta Pharmaceutica Sinica | 2024, 59(1) : 25 - 34
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Acta Pharmaceutica Sinica | 2024, 59(1): 25-34
• Reviews •
The evolution and application progress of non-modified drug target discovery CETSA technology
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Guang-yuan LIU, Ya-hui LI, Wei ZHANG*, De-zhi KONG*
Affiliations
  • Institute of Integrated Traditional Chinese and Western Medicine, Hebei Medical University, Shijiazhuang 050017, China
Published: 2024-01-12 doi: 10.16438/j.0513-4870.2023-0415
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Understanding the research methods for drug protein targets is crucial for the development of new drugs, clinical applications of drugs, drug mechanisms, and the pathogenesis of diseases. Cellular thermal shift assay (CETSA), a target research method without modification, has been widely used since its development. Now, there are various CETSA-based technology combinations, such as mass spectrometry-based cellular thermal shift assay (MS-CETSA), isothermal dose response-cellular thermal shift assay (ITDR-CETSA), amplified luminescent proximity homogeneous assay-cellular thermal shift assay (Alpha-CETSA), etc., which combine their respective advantages and further expand the application scope of CETSA. These technologies are suitable for the entire drug development chain, from drug screening to monitoring the target binding and off-target toxicity of drugs in patients. Based on the author's research experience, this paper reviews the principles of CETSA and related binding technologies, their application in target discovery, and the progress of data processing and analysis in recent years, aiming to provide reference and reference for the further application of CETSA.

cellular thermal shift assay  /  thermal proteome profiling  /  target discovery  /  technology combination
Guang-yuan LIU, Ya-hui LI, Wei ZHANG, De-zhi KONG. The evolution and application progress of non-modified drug target discovery CETSA technology[J]. Acta Pharmaceutica Sinica, 2024 , 59 (1) : 25 -34 . DOI: 10.16438/j.0513-4870.2023-0415
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doi: 10.16438/j.0513-4870.2023-0415
  • Receive Date：2023-04-06
  • Online Date：2025-11-28
  • Published：2024-01-12
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  • Received：2023-04-06
  • Revised：2023-07-17
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    Institute of Integrated Traditional Chinese and Western Medicine, Hebei Medical University, Shijiazhuang 050017, China
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