Affinity Mass Spectrometry-Based Fragment Screening Identified a New Negative Allosteric Modulator of the Adenosine A<sub>2A</sub> Receptor Targeting the Sodium Ion Pocket
Yan Lu, Hongyue Liu, Dehua Yang, Zhong‐Guang Li, Xin Ye, Suwen Zhao, Ming‐Wei Wang, Qingtong Zhou, Wenqing Shui
Abstract
AR. Taken together, our work would facilitate fragment-based screening of allosteric modulators, as well as guide the design of novel NAMs acting at the sodium ion pocket of class A GPCRs.
Topics & Concepts
Allosteric regulationG protein-coupled receptorChemistryAllosteric modulatorLigand (biochemistry)Surface plasmon resonanceSmall moleculeReceptorAdenosine receptorStereochemistryBiophysicsBiochemistryAgonistBiologyNanotechnologyNanoparticleMaterials scienceReceptor Mechanisms and SignalingNeuropeptides and Animal PhysiologyMass Spectrometry Techniques and Applications