A High Throughput Assay For Discovering New Inhibitors of the GIRK1/4 Channel


Reference #: 00792

Invention Description:

Discovery of new drugs that act on the cardiac IK,Ach has been hampered by the absence of a cell-based high throughput screening system that utilizes IK,Ach. The present invention provides a high throughput methodology for discovering new drugs that bind to and inhibit IK,Ach. In this invention, cells expressing IK,Ach are plated in 96-well culture dishes and treated with potential drugs that inhibit IK,Ach. The activity of IK,Ach is then measured in the presence of muscarinic agent carbachol using a fluorescent imaging plate reader (FLIPR).

Potential Applications:

Atrial fibrillation (AF) is the most commonly occurring cardiac arrhythmia and is responsible for significant morbidity, mortality and health care costs. The incidence of AF is expected to increase markedly with the aging U.S. population. However, the use of conventional anti-arrhythmic drugs for treating AF has been limited due to their toxic actions. One novel target for AF drug therapy is the acetylcholine-activated K+ channel (IK,Ach). This protein is found in the plasma membrane of the cells that make up the heart and forms a pore or channel that allows K+ movement into and out of the cells. IK,Ach opens upon binding of hormones such as acetylcholine to the cardiac muscarinic (M2) receptor and regulates the heart rate and contraction.

Advantages and Benefits:

This technique brings a novel tool to the medical community in combating AFs. With yet another way to treat AFs, health care costs could be decreased. More importantly, by detecting the dangerous condition of AF, doctors can quickly and accurately diagnose the problem and prescribe treatment, potentially saving many lives.

Patent Information:
Title App Type Country Serial No. Patent No. File Date Issued Date Expire Date Patent Status
High Throughput Assay For Discovering New Inhibitors of the GIRK1/4 Channel Utility United States 13/107,351 8,323,911 5/13/2011 12/4/2012 5/13/2031 Issued
For Information, Contact:
Technology Commercialization
University of South Carolina
Kenneth Walsh
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