Conformation state-sensitive antibodies to G-protein-coupled receptors.

ABSTRACT: A growing body of evidence indicates that G-protein-coupled receptors undergo complex conformational changes upon agonist activation. It is likely that the extracellular region, including the N terminus, undergoes activation-dependent conformational changes. We examined this by generating antibodies to regions within the N terminus of micro-opioid receptors. We find that antibodies to the midportion of the N-terminal tail exhibit enhanced recognition of activated receptors, whereas those to the distal regions do not. The enhanced recognition is abolished upon treatment with agents that block G-protein coupling or deglycosylate the receptor. This suggests that the N-terminal region of mu receptors undergoes conformational changes following receptor activation that can be selectively detecte

SUBMITTER: Gupta A 

PROVIDER: S-EPMC3856726 | biostudies-literature | 2007 Feb

REPOSITORIES: biostudies-literature