What is SGK1 & Selective Inhibition?

Serum and Glucocorticoid Kinase 1 (SGK1) is a protein kinase, which regulates a number of ion currents in human cardiac cells, and works to support cell survival and proliferation in many resistant cancer cells.

Cardiomyocytes

Cardiomyocytes are specialized cells found in the heart muscle that are responsible for the contraction and relaxation of the heart.

Overactivity of SGK1 has been linked to both cardiac ion channel effects as well as a mediator of fibrotic and inflammatory signaling. SGK1-mediated cardiac ion channel effects result in adverse prolongation of the QT interval in animals and humans leading to both Congenital and Acquired (Drug-Induced) Long QT Syndrome - both of which can lead to the development of lethal arrhythmias. Increased fibrotic and inflammatory signaling due to upregulated SGK1 activity in metabolic disease plays a significant role in the development of atrial fibrillation and heart failure. We are investigating our selective and novel SGK1 inhibitors as therapeutics to modulate ion channel activity in Long QT Syndrome and fibrotic and inflammatory signaling in atrial fibrillation and heart failure.