Robust Multiplex Mass Spectrometric Assay for Screening Small-Molecule Inhibitors
A robust multiplex mass spectrometric assay for screening small-molecule inhibitors of CD73 with diverse inhibition modalities. Credit: Gejing Deng
A new original research article in SLAS Discovery presents a fast, sensitive, and robust methodology for screening small molecule inhibitors against CD73/Ecto-5'-Nucleotidase, a promising target for developing anti-cancer drugs.
The methodology described by authors Gejing Deng (Sanofi) et al., uses multiple stable isotope-labeled substrates for carrying out CD73 reactions followed by sample pooling then simultaneously quantifying multiple reaction products using ultra-fast RapidFire-MS/MS.
In contrast to other optical based methodologies, this methodology allows identifying molecules with diverse inhibition modalities and characterizing inhibitors using both recombinant CD73 and CD73+ cells.
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