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Development of an Affinity-Based Probe to Profile Endogenous Human Adenosine A3Receptor Expression

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Title: Development of an Affinity-Based Probe to Profile Endogenous Human Adenosine A3Receptor Expression
Authors: Beerkens, Bert L. H., Snijders, Inge M., Snoeck, Joep, Liu, Rongfang, Tool, Anton T. J., Le Dévédec, Sylvia E., Jespers, Willem, Kuijpers, Taco W., van Westen, Gerard J.P., Heitman, Laura H., IJzerman, Adriaan P., van der Es, Daan
Source: Journal of Medicinal Chemistry; August 2023, Vol. 66 Issue: 16 p11399-11413, 15p
Abstract: The adenosine A3receptor (A3AR) is a G protein-coupled receptor (GPCR) that exerts immunomodulatory effects in pathophysiological conditions such as inflammation and cancer. Thus far, studies toward the downstream effects of A3AR activation have yielded contradictory results, thereby motivating the need for further investigations. Various chemical and biological tools have been developed for this purpose, ranging from fluorescent ligands to antibodies. Nevertheless, these probes are limited by their reversible mode of binding, relatively large size, and often low specificity. Therefore, in this work, we have developed a clickable and covalent affinity-based probe (AfBP) to target the human A3AR. Herein, we show validation of the synthesized AfBP in radioligand displacement, SDS-PAGE, and confocal microscopy experiments as well as utilization of the AfBP for the detection of endogenous A3AR expression in flow cytometry experiments. Ultimately, this AfBP will aid future studies toward the expression and function of the A3AR in pathologies.
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  Data: Development of an Affinity-Based Probe to Profile Endogenous Human Adenosine A3Receptor Expression
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  Data: Journal of Medicinal Chemistry; August 2023, Vol. 66 Issue: 16 p11399-11413, 15p
– Name: Abstract
  Label: Abstract
  Group: Ab
  Data: The adenosine A3receptor (A3AR) is a G protein-coupled receptor (GPCR) that exerts immunomodulatory effects in pathophysiological conditions such as inflammation and cancer. Thus far, studies toward the downstream effects of A3AR activation have yielded contradictory results, thereby motivating the need for further investigations. Various chemical and biological tools have been developed for this purpose, ranging from fluorescent ligands to antibodies. Nevertheless, these probes are limited by their reversible mode of binding, relatively large size, and often low specificity. Therefore, in this work, we have developed a clickable and covalent affinity-based probe (AfBP) to target the human A3AR. Herein, we show validation of the synthesized AfBP in radioligand displacement, SDS-PAGE, and confocal microscopy experiments as well as utilization of the AfBP for the detection of endogenous A3AR expression in flow cytometry experiments. Ultimately, this AfBP will aid future studies toward the expression and function of the A3AR in pathologies.
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        Value: 10.1021/acs.jmedchem.3c00854
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        Text: English
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            – D: 24
              M: 08
              Text: August 2023
              Type: published
              Y: 2023
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