Exploring the activation pathway and G_i-coupling specificity of the μ-opioid receptor.

ABSTRACT: Understanding the activation mechanism of the μ-opioid receptor (μ-OR) and its selective coupling to the inhibitory G protein (G_i) is vital for pharmaceutical research aimed at finding treatments for the opioid overdose crisis. Many attempts have been made to understand the mechanism of the μ-OR activation, following the elucidation of new crystal structures such as the antagonist- and agonist-bound μ-OR. However, the focus has not been placed on the underlying energetics and specificity of the activation process. An energy-based picture would not only help to explain this coupling but also help to explore why other possible options are not common. For example, one would like to understand why μ-OR is more selective to G_i than a stimulatory G protein (G_s).

SUBMITTER: Mondal D 

PROVIDER: S-EPMC7585030 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature