Article
The second extracellular loop of GPCRs determines subtype-selectivity and controls efficacy as evidenced by loop exchange study at A2 adenosine receptors.
Biochemical pharmacology - 1 May 2013
Seibt Benjamin F, Schiedel Anke C, Thimm Dominik, Hinz Sonja, Sherbiny Farag F, Müller Christa E
Abstract excerpt
The second extracellular loop (EL2) of G protein-coupled receptors (GPCRs), which represent important drug targets, may be involved in ligand recognition and receptor activation. We studied the closely related adenosine receptor (AR) subtypes A2A and A2B by exchanging the complete EL2 of the human A2BAR for the EL2 of the A2AAR. Furthermore, single amino acid residues (Asp148(45.27), Ser149(45.28), Thr151(45.30),...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.