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US 2011/0212461 A1Published application
Prediction of cardiotoxicity
OwnerHans Marcus Ludwig Bitter, Kyle Louis Kolaja +3inventors
InventorsHans Marcus Ludwig Bitter, Kyle Louis Kolaja, Preeti Dhawan, Hirdesh Uppal, Nina Gonzaludo
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Abstract
The likelihood that a compound will exhibit cardiotoxicity in an in vitro or in vivo assay predicted by the ability of the compound to inhibit at least one kinase from a selected group.
Claims12
A method for predicting the cardiotoxicity of a compound, said method comprising:
- a) providing a test compound;
- b) determining the ability of the compound at a concentration of about 10 μM to inhibit the kinase activity in the model kinase group consisting of CSF1R, KIT, FYN, PDGFR beta, FGR, LCK, Ephrin Receptor B1, FRK, ABL1, PDGFR alpha, and HCK, wherein inhibition by over 80% of at least one of said kinases indicates a likelihood that said test compound will demonstrate cardiotoxicity.
A method for screening compounds for potential cardiotoxicity, said method comprising:
- a) providing a plurality of test compounds;
- b) determining the ability of each compound at 10 μM concentration to inhibit the kinase activity in the model kinase group consisting of CSF1R, KIT, FYN, PDGFR beta, FGR, LCK, Ephrin Receptor B1, FRK, ABL1, PDGFR alpha, and HCK, wherein inhibition by over 80% of at least one of said kinases indicates a likelihood that said test compound will demonstrate cardiotoxicity;
- c) rejecting compounds that demonstrate a likelihood of cardiotoxicity.
A test substrate, comprising:
- A solid support;
- and
- Immobilized on said solid support, the kinases CSF1R, KIT, FYN, PDGFR beta, FGR, LCK, Ephrin Receptor B1, FRK, ABL1, PDGFR alpha, and HCK.
Dependencies are inferred from the claim text.