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US 2006/0136140 A1Published application
Method for identification and functional characterization of agents which modulate ion channel activity
OwnerScott Perschke, Ming Liuinventors
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Abstract
Materials, methods and a computer system are provided which facilitate the identification and characterization of modulators of potassium ion channels, particularly the HERG channel.
Claims28
A method for identifying test compounds which modulate potassium channel activity, comprising;
- a) assembling a dataset of agents known to modulate potassium channel activity, wherein said dataset contains biophysical and structural features of said agents which include observed biological effects of said agents on potassium channel activity;
- b) providing a series of algorithms which describe the interaction of said structural features with said potassium channel;
- c) assessing the test compound for the presence or absence of the structural features of a) using the algorithms of b), thereby identifying test compounds sharing structural features with said agents which also modulate potassium channel activity.
A functional cell based assay for identifying test compounds suspected of modulating HERG protein activity via interaction at the E4031 site, comprising:
- a) contacting HERG expressing cells with said test compound and determining the effects of said test compound on HERG channel function as compared to
- i) cells which do not express HERG;
- ii) HERG expressing cells which had not been exposed to said test compound;
- and
- iii) cells exposed to E4031.
2 more elements
An in vitro assay for determining a test compound's binding affinity for the E-4031 site on HERG protein or a fragment thereof, comprising:
- a) providing HERG protein or a fragment thereof;
- b) detectably labeling a test compound which binds HERG at said E4031 site;
- c) performing a competitive binding assay with said detectably labeled test compound in the presence and absence of test compound that has not been detectably labeled, thereby determining the binding affinity of said test compound for said 4031 site on said HERG protein.
Dependencies are inferred from the claim text.