Development of an Affinity-Based Probe to Profile Endogenous Human Adenosine A₃ Receptor Expression.

ABSTRACT: The adenosine A₃ receptor (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

SUBMITTER: Beerkens BLH 

PROVIDER: S-EPMC10461224 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature