Conformationally selective RNA aptamers allosterically modulate the β2-adrenoceptor.

ABSTRACT: G-protein-coupled receptor (GPCR) ligands function by stabilizing multiple, functionally distinct receptor conformations. This property underlies the ability of 'biased agonists' to activate specific subsets of a given receptor's signaling profile. However, stabilizing distinct active GPCR conformations to enable structural characterization of mechanisms underlying GPCR activation remains difficult. These challenges have accentuated the need for receptor tools that allosterically stabilize and regulate receptor function through unique, previously unappreciated mechanisms. Here, using a highly diverse RNA library combined with advanced selection strategies involving state-of-the-art next-generation sequencing and bioinformatics analyses, we identify RNA aptamers that bind a prototypical GPC

SUBMITTER: Kahsai AW 

PROVIDER: S-EPMC4990464 | biostudies-literature | 2016 Sep

REPOSITORIES: biostudies-literature