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October 2, 2025Journal of Medicinal Chemistry

Bitopic A3 Adenosine Receptor Molecular Probes: Positive Allosteric Modulation and Noncanonical Activation

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Authors

SKSiva Hariprasad KurmaMPMatteo PavanTWTina C. Wan

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Overview

Assessment shows enhanced agonist potency and efficacy in A3 adenosine receptors, indicating novel bitopic molecular probes.

Key Points

  • The novel compounds achieved about 300% maximal agonist efficacy, enhancing activation of the A3 adenosine receptor.
  • Substitutions like 4-methyl and 4-iodo enhanced agonist potency by up to 30.5-fold, highlighting structural modifications.
  • Molecular dynamics simulations revealed stable interactions with phospholipids, supporting A3 adenosine receptor allosteric binding.
  • Optimizing the structure-activity relationship of bitopic modulators indicates potential for developing targeted molecular probes.

Cite This Study

Kurma et al. (2025) studied this question.

synapsesocial.com/papers/68de8eaeaa6cec72c69ea7a3https://doi.org/10.1021/acs.jmedchem.5c01985
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