Resonant waveguide grating based assays for colloidal aggregate detection and promiscuity characterization in natural products.

ABSTRACT: Small molecules, including natural compounds, in aqueous buffer that self-associate into colloidal aggregates is the main cause of false results in the early stage of drug discovery. Here we reported resonant waveguide grating (RWG) based assays to identify natural compound aggregation and characterize its influence on membrane receptors in living cells. We first applied a cell-free aggregation assay to determine compound critical aggregation concentration (CAC) values. Then we characterized the aggregators' influence on membrane receptors using three types of dynamic mass redistribution (DMR) assays. Results showed that colloidal aggregates may cause false activity in DMR desensitization assays; some of the false activities can be implied by the large response in DMR agonism assays and ca

SUBMITTER: Wang R 

PROVIDER: S-EPMC9075791 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature