Development of a Conformational Histamine H₃ Receptor Biosensor for the Synchronous Screening of Agonists and Inverse Agonists.

ABSTRACT: The histamine H₃ receptor (H₃R) represents a highly attractive drug target for the treatment of various central nervous system disorders, but the discovery of novel H₃R targeting compounds relies on the assessment of highly amplified intracellular signaling events that do not only reflect H₃R modulation and carry the risk of high false-positive and -negative screening rates. To address these limitations, we designed an intramolecular H₃R biosensor based on the principle of bioluminescence resonance energy transfer (BRET) that reports the receptor's real-time conformational dynamics and provides an advanced tool to screen for both H₃R agonists and inverse agonists in a live cell screening-compatible assay format. This conform

SUBMITTER: Schihada H 

PROVIDER: S-EPMC7325232 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature