Modulatory binding site in potassium channels for screening and finding new active ingredients
AssigneeArzneimittelwerk Dresden GmbH
InventorsChris Rundfeldt, Rainer Netzer
Life of this patent
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Abstract
A selective modulatory retigabine binding potassium channel receptor site containing subunits KCNQ2 and KCNQ3, and a method for directly selectively modulating that receptor site by administering retigabine to a cell preparation of the potassium channel.
Claims11
A method for identifying a compound which positively or negatively modulates a potassium channel comprising KCNQ2 or KCNQ2 and KCNQ3 subunits, the method comprising
- (a) providing a cell culture containing the genetic information for producing the KCNQ2 subunit alone, or in combination with the subunit KCNQ3, and translating the information into a functional protein;
- (b) adding to said protein (i) a substance to be tested;
- and (ii) a reporter system indicating an activation or inactivation of the channel;
- and
- (c) observing the effect of the substance to be tested in comparison to addition of retigabine to said protein and reporter system.
A method for identifying a compound which positively or negatively modulates a potassium channel comprising KCNQ2 or KCNQ2 and KCNQ3 subunits, the method comprising
- (a) providing an artificially produced cell-like construct with a functionally embedded potassium channel containing at least KCNQ2 OR KCNQ2 and KCNQ3 subunits functionally embedded into said construct;
- (b) adding to said construct (i) a substance to be tested;
- and (ii) a reporter system indicating an activation or inactivation of the channel;
- and
- (c) observing the effect of the substance to be tested in comparison to addition of retigabine to said protein and reporter system.
A method for identifying a compound binding to the retigabine binding site of the potassium channel comprising KCNQ2 or KCNQ2 and KCNQ3 subunits, the method comprising
- (a) providing a cell culture containing the genetic information for producing the KCNQ2 subunit alone, or in combination with the subunit KCNQ3, and translating the information into a functional protein;
- (b) adding to said protein (i) unlabeled retigabine, (ii) labeled retigabine and (iii) the substance to be tested under conditions used for a competitive binding assay, and
- (c) determining whether the substance to be tested competes with retigabine for the retigabine binding site on the potassium channel.
A method for identifying a compound binding to the retigabine binding site of the potassium channel comprising of KCNQ2 or KCNQ2 and KCNQ3 subunits, the method comprising
- (a) providing an artificially produced cell-like construct with a functionally embedded potassium channel containing at least KCNQ2 or KCNQ2 and KCNQ3 subunits functionally incorporated into said construct;
- (b) adding to said protein (i) retigabine, (ii) labeled retigabine and (iii) the substance to be tested under conditions used for a competitive binding assay, and
- (c) determining whether the substance to be tested competes with the retigabine for the retigabine binding site on the potassium channel.
Dependencies are inferred from the claim text.