Discovery of Potent and Selective Methylenephosphonic Acid CD73 Inhibitors
Ehesan U. Sharif, Jarosław Kalisiak, Kenneth V. Lawson, Dillon H. Miles, Eric T. Newcomb, Erick A. Lindsey, Brandon R. Rosen, Laurent Debien, Ada Chen, Xiaoning Zhao, Stephen W. Young, Nigel P.C. Walker, Norbert Sträter, Emma Rose Scaletti, Lixia Jin, Guifen Xu, Manmohan R. Leleti, Jay P. Powers
Abstract
, which exhibits excellent potency against CD73, exquisite selectivity against related ectonucleotidases, and a favorable pharmacokinetic profile.
Topics & Concepts
ChemistryAdenosineAdenosine receptorATP hydrolysisBiochemistryPharmacologyPurinergic signallingExtracellularImmune systemEnzymeReceptorAgonistImmunologyBiologyATPaseAdenosine and Purinergic SignalingClick Chemistry and ApplicationsSynthesis and Biological Evaluation