Discovery of a Series of Potent, Selective, and Orally Bioavailable Nucleoside Inhibitors of CD73 That Demonstrates In Vivo Antitumor Activity
Li J, Chen L, Billedeau R, Stanton T, Chiang J, Lee C, Li W, Steggerda S, Emberley E, Gross M, Bhupathi D, Che X, Chen J, Dang R, Huang T, Ma Y, MacKinnon A, Makkouk A, Marguier G, Neou S, Sotirovska N, Spurlock S, Zhang J, Zhang W, van Zandt M, Yuan L, Savoy J, Parlati F, Sjogren E. Discovery of a Series of Potent, Selective, and Orally Bioavailable Nucleoside Inhibitors of CD73 That Demonstrates In Vivo Antitumor Activity. Journal Of Medicinal Chemistry 2022, 66: 345-370. PMID: 36529947, DOI: 10.1021/acs.jmedchem.2c01287.Peer-Reviewed Original ResearchConceptsSuppression of CD8<sup>+</sup> T cellsCD8<sup>+</sup> T cellsAdenosine monophosphateSmall-molecule CD73 inhibitorsMouse tumor modelsEcto-5'-nucleotidaseAntitumor mechanism of actionCheckpoint inhibitorsCancer immunotherapyImmunosuppressive adenosineInhibitors of CD73Mechanism of actionT cellsCD73 activityTumor modelTumor progressionHydrolysis of adenosine monophosphateDose-dependentlyCancer patientsCD73 inhibitorsOral administrationAntitumor activityCD73CancerSerum samples
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