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MALDI-TOF Mass Spectrometry-Based Assay for Measuring Covalent Target Engagement of KRAS G12C Inhibitors

  1. Author:
    Dyba,Marcin
    Denson,John-Paul
    Maciag,Anna

  2. Author Address

    NCI RAS Initiative, Cancer Research Technology Program, Frederick National Laboratory for Cancer Research, Frederick, MD, USA. marcin.dyba@nih.gov.,
    1. Year: 2024
  2. Journal: Methods in Molecular Biology (Clifton, N.J.)
    1. 2797
    2. Pages: 145-157
  4. Type of Article: Article
  1. Abstract:

    MALDI-TOF mass spectrometry enables high-throughput screening of covalent fragment libraries and SAR compound progressions of selective KRAS G12C inhibitors. Using the MALDI-TOF platform instead of the more traditional ESI-MS TOF/orbitrap instrumentation can radically shorten sample acquisition time, allowing up to 384 samples to be screened in 30 min. The typical throughput for a covalent library screen is 1152 samples per 8 h, including processing, calculation, and reporting steps. The throughput can be doubled without any significant assay modification. © 2024. The Author(s), under exclusive license to Springer Science+Business Media, LLC, part of Springer Nature.

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External Sources

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  2. DOI: 10.1007/978-1-0716-3822-4_11
  3. PMID: 38570458

Library Notes

  1. Fiscal Year: FY2023-2024
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