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• W3117282943 abstract "Small-molecules acting as positive allosteric modulators (PAMs) of the A2B adenosine receptor (A2B 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 A2B 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 A2B AR." @default.
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• W3117282943 date "2020-12-17" @default.
• W3117282943 modified "2023-10-16" @default.
• W3117282943 title "Novel positive allosteric modulators of A_2B adenosine receptor acting as bone mineralisation promoters" @default.
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• W3117282943 doi "https://doi.org/10.1080/14756366.2020.1862103" @default.
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