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April 13, 2026ACS Chemical Biology

An Integrative Biophysical and Computational Workflow Uncovers New Allosteric Sites and Modulators of the Human A 2A Adenosine Receptor

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Authors

RPRenaud PrudentARArka Prabha RayUniversity of FloridaNTNaveen ThakurUniversity of Florida

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Overview

Uncovers novel allosteric modulators of the A2A adenosine receptor, suggesting new therapeutic avenues.

Key Points

  • This research aims to identify and characterize novel allosteric modulators of the human A2A adenosine receptor.
  • Employed affinity selection-mass spectrometry (AS-MS) with a diverse chemical library.
  • Conducted competition binding and orthogonal biophysical assays to confirm allostericity.
  • Integrated computational workflow to predict allosteric sites and model ligand interactions.
  • Identified multiple allosteric modulators that influence cAMP production despite weak affinity.
  • Classified these compounds as negative allosteric modulators (NAMs) with unique pharmacological profiles.
  • Revealed previously unknown intracellular and extracellular allosteric sites.

Cite This Study

Prudent et al. (2026) studied this question.

synapsesocial.com/papers/69dc88303afacbeac03ea171https://doi.org/10.1021/acschembio.6c00003
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