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Rubiscolins are naturally occurring G protein-biased delta opioid receptor peptides.


ABSTRACT: The impact that β-arrestin proteins have on G protein-coupled receptor trafficking, signaling and physiological behavior has gained much appreciation over the past decade. A number of studies have attributed the side effects associated with the use of naturally occurring and synthetic opioids, such as respiratory depression and constipation, to excessive recruitment of β-arrestin. These findings have led to the development of biased opioid small molecule agonists that do not recruit β-arrestin, activating only the canonical G protein pathway. Similar G protein-biased small molecule opioids have been found to occur in nature, particularly within kratom, and opioids within salvia have served as a template for the synthesis of other G protein-biased opioids. Here, we present the first report

SUBMITTER: Cassell RJ 

PROVIDER: S-EPMC6421079 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature