Abstract
This study compared detergent-solubilised (soluble) and lipid-reconstituted (proteoliposome) protein to establish a high-throughput method for identifying membrane protein inhibitors. We identified inhibitors of the membrane-bound type II NADH dehydrogenase with lower lipophilicity and better potency, suggesting proteoliposome systems may be advantageous over detergent-solubilised systems for respiratory membrane proteins.
•Purified respiratory Type II NADH dehydrogenase (NDH-2) was lipid-reconstituted.•Detergent-solubilised and lipid-reconstituted NDH-2 was screened for inhibitors.•Inhibitors of lipid-reconstituted NDH-2 were more potent and less lipophilic.•Lipid-reconstituted respiratory membrane-protein drug-screening may be advantageous.