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A Robust Multiplex Mass Spectrometric Assay for Screening Small-Molecule Inhibitors of CD73 with Diverse Inhibition Modalities

SLAS News (Jan. 17, 2018) — 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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A Robust Multiplex Mass Spectrometric Assay for Screening Small-Molecule Inhibitors of CD73 with Diverse Inhibition Modalities can be accessed for free at http://journals.sagepub.com/doi/full/10.1177/2472555217750386. For more information about SLAS and its journals, visit www.slas.org/journals.

 

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