What is it about?

Blockage of the circulation in a non-fatal heart attack produces damaged heart cells and a tendency to generate arrhythmias. There is no reliable therapy for this. In the heart there are ion channels activated by mechanical stress that can leak calcium into the cells leading to atrophy and death. By blocking these channels we can reduce the damage and the arrhythmias. The inhibitor is called gsmtx4 and is a small peptide that is non allergenic, nontoxic, produced chemically by drug company standards, and it has a long half life in the body meaning that drug administration frequency is minimized.

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Why is it important?

GsMtx4 is the only known specific inhibitor of mechanosensitive ion channels and its structure and mechanism of action are well known. It is active in the D and L forms showing that it acts in non traditional ways. We are pursuing its application to muscular dystrophy since that genetic disease leads to activation of these ion channels. It is noted as an orphan drug by the FDA and is approaching submission of an IND, and investigative new drug, to the FDA. This drug promises not only to relieve atrophy of the skeletal muscles but also reduce the risk of cardiac failure, the most common cause of death in muscular dystrophy.

Perspectives

This is the first publication showing the pharmacokinetics of GsMtx4, the lack of effect on the EKG of normal free roaming animals, the reduction in cardiac damage from repersuion and infarct and the suppression of arrhythmias associated with reperfusion.

Dr Frederick Sachs
suny

Read the Original

This page is a summary of: GsMTx4-D is a cardioprotectant against myocardial infarction during ischemia and reperfusion, Journal of Molecular and Cellular Cardiology, September 2016, Elsevier,
DOI: 10.1016/j.yjmcc.2016.07.005.
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