Agonist bias and agonist-dependent antagonism at corticotrophin releasing factor receptors.

ABSTRACT: The corticotropin-releasing factor (CRF) receptors represent potential drug targets for the treatment of anxiety, stress, and other disorders. However, it is not known if endogenous CRF receptor agonists display biased signaling, how effective CRF receptor antagonists are at blocking different agonists and signaling pathways or how receptor activity-modifying proteins (RAMPs) effect these processes. This study aimed to address this by investigating agonist and antagonist action at CRF₁ and CRF₂ receptors. We used CRF₁ and CRF₂ receptor transfected Cos7 cells to assess the ability of CRF and urocortin (UCN) peptides to activate cAMP, inositol monophosphate (IP₁ ), and extracellular signal-regulated kinase 1/2 signaling and determined th

SUBMITTER: Tasma Z 

PROVIDER: S-EPMC7290078 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature