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Cited by 6Adenosine and Purinergic SignalingClick Chemistry and ApplicationsReceptor Mechanisms and Signaling

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Development of an Affinity-Based Probe to Profile Endogenous Human Adenosine A 3 Receptor Expression

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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·2023·Journal of Medicinal Chemistry
DOI 10.1021/acs.jmedchem.3c00854PMC PMC10461224

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Abstract

High Resolution Image Download MS PowerPoint Slide The adenosine A 3 receptor (A 3 AR) 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 A 3 AR 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 A 3 AR. 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 A 3 AR expression in flow cytometry experiments. Ultimately, this AfBP will aid future studies toward the expression and function of the A 3 AR in pathologies.

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Metadata

Authors
Beerkens, B. L. H., Snijders, I. M., Snoeck, J., Liu, R., Tool, A. T. J., Le Dévédec, S. E., Jespers, W., Kuijpers, T. W., van Westen, G. J. P., Heitman, L. H., IJzerman, A. P., & van der Es, D.
Affiliations
  • Leiden University (NL)
  • Sanquin (NL)
  • Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands
  • Amsterdam UMC Location University of Amsterdam (NL)
Corresponding author
van der Es, Daan
ORCID
Venue
Journal of Medicinal Chemistry
Publisher
American Chemical Society (ACS)
Published
2023-08-02
Volume
66
Issue
16
Pages
11399-11413
ISSN
  • 0022-2623 (ISSN-L)
  • 1520-4804
DOI
10.1021/acs.jmedchem.3c00854
PMC
PMC10461224
OpenAlex
W4385487808
Cited by
6
References
1
Citations by year
2026: 1 · 2025: 3 · 2024: 2
FWCI
1.12
Type
journal article
Language
en
Open access
Licence
Locations
  • Journal of Medicinal Chemistry (publishedVersion, cc-by)
  • ChemRxiv (acceptedVersion, cc-by-nc-nd)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • Leiden Repository (Leiden University) (submittedVersion, cc-by)
  • Pure Amsterdam UMC (submittedVersion, cc-by)
Funders
  • Universiteit Leiden
  • Universiteit van Amsterdam
  • Oncode Institute
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Physiology › Adenosine and Purinergic Signaling
  • Physical Sciences › Chemistry › Organic Chemistry › Click Chemistry and Applications
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Keywords
A3 adenosine receptor, G protein-coupled receptors, covalent probes, radioligand binding, flow cytometry detection, confocal microscopy, immunomodulation
MeSH terms
Adenosine, Humans, Gene Expression, Receptors, G-Protein-Coupled, Receptor, Adenosine A3, Adenosine A3 Receptor Agonists

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