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March 18, 2026Medicinal Chemistry ResearchOpen Access

From empirical screening to lipid trolling: the evolution of extrahelical allosteric modulators of A1 and A3 adenosine receptors

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Authors

MPMatteo PavanSKSiva Hariprasad KurmaPOPaola Oliva

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Overview

This research shows enhanced agonist effects and receptor modulation through lipid-exposed sites in adenosine receptors, suggesting new treatment pathways.

Key Points

  • The study aims to explore the development of allosteric modulators for A1 and A3 adenosine receptors and their therapeutic potential.
  • Utilized cryo-EM studies for structural assessment of receptor binding sites.
  • Employed mutagenesis and molecular modeling for PAM discovery.
  • Conducted synthetic optimization to improve pharmacological profiles of PAMs.
  • Applied molecular dynamics simulations to predict lipid interactions with PAMs.
  • Identified effective PAMs that enhance agonist potency at A1 and A3 adenosine receptors.
  • Demonstrated the role of lipid-exposed binding sites in improving drug characteristics.
  • Showed that PAMs can activate receptors even without orthosteric agonists.

Cite This Study

Pavan et al. (2026) studied this question.

synapsesocial.com/papers/69ba43584e9516ffd37a477ehttps://doi.org/10.1007/s00044-026-03534-5
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