Edward N. Harris
Lincoln, Nebraska 68588-0664
Editorial
Heparin Clearance by Liver Scavenger Receptors
Author(s): Edward N. HarrisEdward N. Harris
The range of assay technologies for the binding and signaling has been developed in HTS laboratories for the identification of hit or lead compounds acting on GPCRs. The [35S] GTPγS binding assay still remains to be a useful and simple technique to demonstrate receptor activation and is one of the few functional, cell-free assays. However, its radioactive nature imposes clear limitations to its use in regular laboratory practice and in high-throughput experimentations. Herein, we have developed a new non-radioactive version of the assay using europium-labeled GTP analogue in which europium-GTP binding can be assayed using time-resolved fluorescence. In continuation with our efforts, this assay was adapted for Histamine 3 receptors. The assay format was specifically evaluated by testing known histamine 3 agonists (Imetit, Immepip, Methylhistamine, Proxifan and Histamine) and anta.. View More»
DOI:
10.4172/2161-1009.1000e114