High-throughput screening assay for mitochondrially-active drugs

Brief interruptions of coronary blood flow paradoxically protect the heart from subsequent prolonged ischemia. The basis of such endogenous cardioprotection, known as "ischemic preconditioning," remains uncertain. Pharmacological evidence has implicated ATP-dependent potassium (KATP) channels in the mechanism of preconditioning; however, it has not been clear whether the sarcolemmal or inner mitochondrial potassium channels are involved in this protection. Results from the Marban laboratory have demonstrated that the inner mitochondrial K+ channels alone mediate this ischemic preconditioning, and that the activity of these inner mitochondrial channels can be selectively modulated. Description (Set) Proposed Use (Set) The novel experimental approach used to determine the inner mitochondrial channels? role in ischemic preconditioning can be exploited in an assay which identifies candidate cardioprotective drugs. This assay exploits a natural fluorescent phenomenon in the mitochondria and is adaptable to a variety of assay platforms. A lead compound is known: therefore, the project is amenable to focussed library screening
Patent (Set) 6,183,948; 6,586,241;

Patents:
US 6,183,948

Inventor(s): Marban, Eduardo

Type of Offer: Licensing



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