Identification of V6.51L as a selectivity hotspot in stereoselective A_2B adenosine receptor antagonist recognition.

ABSTRACT: The four adenosine receptors (ARs) A₁AR, A_2AAR, A_2BAR_, and A₃AR are G protein-coupled receptors (GPCRs) for which an exceptional amount of experimental and structural data is available. Still, limited success has been achieved in getting new chemical modulators on the market. As such, there is a clear interest in the design of novel selective chemical entities for this family of receptors. In this work, we investigate the selective recognition of ISAM-140, a recently reported A_2BAR reference antagonist. A combination of semipreparative chiral HPLC, circular dichroism and X-ray crystallography was used to separate and unequivocally assign the configuration of each enantiomer. Subsequently affinity evaluation for both A_2A

SUBMITTER: Wang X 

PROVIDER: S-EPMC8266863 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature