Multiplex mass spec assay for small-molecule inhibitors of CD73 with diverse modalities

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.

More information:
Jessica McManus et al, A Robust Multiplex Mass Spectrometric Assay for Screening Small-Molecule Inhibitors of CD73 with Diverse Inhibition Modalities, SLAS DISCOVERY: Advancing Life Sciences R&D (2018). DOI: 10.1177/2472555217750386

Provided by Society for Laboratory Automation and Screening