Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 36, Issue 1, Pages 286-294Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2020.1862103
Keywords
A(2B) adenosine receptor; allosteric modulators; mesenchymal stem cell; bone formation
Funding
- Italian Ministry of Education [2015E8EMCM_007]
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The study investigated compounds with chemical similarity to known PAMs of A(2B) AR, identifying lead compounds with potential as anti-osteoporosis agents. Further characterization of benzofurane derivative 9 confirmed its role as a PAM of A(2B) AR.
Small-molecules acting as positive allosteric modulators (PAMs) of the A(2B) adenosine receptor (A(2B) AR) could potentially represent a novel therapeutic strategy for pathological conditions characterised by altered bone homeostasis, including osteoporosis. We investigated a library of compounds (4-13) exhibiting different degrees of chemical similarity with three indole derivatives (1-3), which have been recently identified by us as PAMs of the A(2B) AR able to promote mesenchymal stem cell differentiation and bone formation. Evaluation of mineralisation activity of 4-13 in the presence and in the absence of the agonist BAY60-6583 allowed the identification of lead compounds with therapeutic potential as anti-osteoporosis agents. Further biological characterisation of one of the most performing compounds, the benzofurane derivative 9, confirmed that such a molecule behaves as PAM of the A(2B) AR.
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