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Researchers identified new modulators for adenosine receptors (ARs) A2A, A2B, and A3. These compounds, including crisaborole, febuxostat, and paroxetine, are already used clinically for other conditions.

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Area of Science:

  • Pharmacology
  • Medicinal Chemistry
  • Molecular Biology

Background:

  • Adenosine (ADO) is a key extracellular signaling molecule.
  • Adenosine receptors (ARs) A1, A2A, A2B, and A3 are G protein-coupled receptors involved in various physiological functions.
  • ARs are crucial targets for developing drugs for neurological, cardiovascular, inflammatory, and autoimmune diseases.

Purpose of the Study:

  • To identify novel modulators of adenosine receptors (ARs) using a machine learning approach.
  • To investigate the activity of existing drugs as potential AR modulators.

Main Methods:

  • A Bayesian machine learning model was developed and validated using public data for A1AR agonists.
  • Three selected molecules (crisaborole, febuxostat, paroxetine) were tested in vitro.
  • Radioligand binding, β-arrestin, calcium influx, and cAMP assays were performed on HEK293 cells expressing specific AR subtypes.

Main Results:

  • Crisaborole, febuxostat, and paroxetine showed initial in vitro activity at A1AR but lacked confirmation in subsequent assays.
  • Febuxostat and paroxetine inhibited radioligand binding for A2AAR and A3AR.
  • Crisaborole and paroxetine demonstrated agonist activity at A2AAR, with crisaborole also showing weaker activity at A2BAR.
  • Paroxetine exhibited antagonist activity at A3AR.

Conclusions:

  • Novel modulators for A2AAR, A2BAR, and A3AR subtypes were identified.
  • These modulators are clinically used drugs for other indications and possess distinct chemical structures.
  • The findings offer new therapeutic avenues by repurposing existing medications for AR-related conditions.