Label-Free Investigations on the G Protein Dependent Signaling Pathways of Histamine Receptors.

ABSTRACT: G protein activation represents an early key event in the complex GPCR signal transduction process and is usually studied by label-dependent methods targeting specific molecular events. However, the constrained environment of such "invasive" techniques could interfere with biological processes. Although histamine receptors (HRs) represent (evolving) drug targets, their signal transduction is not fully understood. To address this issue, we established a non-invasive dynamic mass redistribution (DMR) assay for the human H_1-4Rs expressed in HEK cells, showing excellent signal-to-background ratios above 100 for histamine (HIS) and higher than 24 for inverse agonists with pEC₅₀ values consistent with literature. Taking advantage of the integrative nature of the DMR assay,

SUBMITTER: Seibel-Ehlert U 

PROVIDER: S-EPMC8467282 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature