Ontology highlight
ABSTRACT:
SUBMITTER: Yang X
PROVIDER: S-EPMC6150691 | biostudies-literature | 2018 Sep
REPOSITORIES: biostudies-literature
Yang Xue X Michiels Thomas J M TJM de Jong Coen C Soethoudt Marjolein M Dekker Niek N Gordon Euan E van der Stelt Mario M Heitman Laura H LH van der Es Daan D IJzerman Adriaan P AP
Journal of medicinal chemistry 20180821 17
Using activity-based protein profiling (ABPP), functional proteins can be interrogated in their native environment. Despite their pharmaceutical relevance, G protein-coupled receptors (GPCRs) have been difficult to address through ABPP. In the current study, we took the prototypical human adenosine A<sub>2A</sub> receptor (hA<sub>2A</sub>R) as the starting point for the construction of a chemical toolbox allowing two-step affinity-based labeling of GPCRs. First, we equipped an irreversibly bindi ...[more]