Discovery of Potent and Selective Non-Nucleotide Small Molecule Inhibitors of CD73
Joel W. Beatty, Erick A. Lindsey, Rhiannon Thomas‐Tran, Laurent Debien, Debashis Mandal, Jenna L. Jeffrey, Anh Tran, Jeremy Fournier, Steven D. Jacob, Xuelei Yan, Samuel L. Drew, Elaine Ginn, Ada Chen, Amber Pham, Sharon Zhao, Lixia Jin, Stephen W. Young, Nigel P.C. Walker, Manmohan R. Leleti, Susanne Moschütz, Norbert Sträter, Jay P. Powers, Kenneth V. Lawson
Abstract
with human CD73 demonstrates a competitive binding mode. These compounds show promise for the improvement of drug-like character via the attenuation of the acidity and low membrane permeability inherent to known nucleoside inhibitors of CD73.
Topics & Concepts
ChemistrySmall moleculeNucleotideStereochemistryStructure–activity relationshipMoleculeBiochemistryIn vitroGeneOrganic chemistryAdenosine and Purinergic SignalingSynthesis and Biological EvaluationNeuropeptides and Animal Physiology