Li, Yulei published the artcileChemical synthesis of a full-Length G-protein-coupled receptor ¦Â2-adrenergic receptor with defined modification patterns at the C-terminus, Category: catalysis-chemistry, the publication is Journal of the American Chemical Society (2021), 143(42), 17566-17576, database is CAplus and MEDLINE.
The ¦Â2-adrenergic receptor (¦Â2AR) is a G-protein-coupled receptor (GPCR) that responds to the hormone adrenaline and is an important drug target in the context of respiratory diseases, including asthma. ¦Â2AR Function can be regulated by post-translational modifications such as phosphorylation and ubiquitination at the C-terminus, but access to the full-length ¦Â2AR with well-defined and homogeneous modification patterns critical for biochem. and biophys. studies remains challenging. Here, we report a practical synthesis of differentially modified, full-length ¦Â2AR based on a combined native chem. ligation (NCL) and sortase ligation strategy. An array of homogeneous samples of full-length ¦Â2ARs with distinct modification patterns, including a full-length ¦Â2AR bearing both monoubiquitination and octaphosphorylation modifications, were successfully prepared for the first time. Using these homogeneously modified full-length ¦Â2AR receptors, we found that different phosphorylation patterns mediate different interactions with ¦Â-arrestin1 as reflected in different agonist binding affinities. Our experiments also indicated that ubiquitination can further modulate interactions between ¦Â2AR and ¦Â-arrestin1. Access to full-length ¦Â2AR with well-defined and homogeneous modification patterns at the C-terminus opens a door to further in-depth mechanistic studies into the structure and dynamics of ¦Â2AR complexes with downstream transducer proteins, including G proteins, arrestins, and GPCR kinases.
Journal of the American Chemical Society published new progress about 71989-31-6. 71989-31-6 belongs to catalysis-chemistry, auxiliary class Amino acide derivatives,pyrrolidine, name is Fmoc-Pro-OH, and the molecular formula is C20H19NO4, Category: catalysis-chemistry.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia