Pharmaceuticals & Vitamin D : Cardiovascular

Pharmaceuticals & Vitamin D Portfolios


New Compounds for Treating High Blood Cholesterol and More

UW–Madison researchers have now developed a method using a rhodium-containing catalyst to make indole compounds, specifically cyclopropyl indoles and cyclohepta[b] indoles. The compounds may be developed into new pharmaceuticals to treat a variety of conditions.

Synthesizing Natural Products to Treat High Blood Cholesterol

UW–Madison researchers have developed an efficient method to synthesize indole compounds, specifically polysubstituted dimeric indoles. These compounds have potential health benefits because they are able to reduce the amount of PCSK9 in cells. PCSK9 is an enzyme known to play a major role in controlling the concentration of LDL cholesterol in the bloodstream.

Some of the compounds have been tested in vitro for their ability to increase the secretion of a potent blood sugar hormone in the body called glucagon-like peptide 1 (GLP-1). Others have the ability to selectively inhibit the secretion of interleukin-17 (IL-17), which is essential in many autoimmune diseases including arthritis, multiple sclerosis, psoriasis and inflammatory bowel disease.

The synthesis process involves a cascade reaction with transition metal catalysts. The resulting compounds can be further functionalized to yield more substituted indoles.

Treating Heart Failure by Inhibiting Myosin Interaction with a Regulatory Myosin Binding Protein

A UW–Madison researcher in collaboration with others has developed peptides for treating and slowing the progression of heart failure. The peptides are designed to disrupt a key interaction involving myosin and Myosin Binding Protein C (MyBP-C).

In healthy hearts, myosin is responsible for generating the force that drives normal cardiac function. It works by continually binding and releasing a protein called actin, in a process that powers heart muscle contractions. In healthy hearts, the process is slowed when myosin is also bound to a regulatory protein, MyBP-C. In compromised hearts, the result of this interaction is to further slow and weaken muscle contractions.

The new peptides target a specific binding site of MyBP-C, thereby blocking attachment to myosin. The peptides could be administered as small-molecule pharmaceuticals in conjunction with other therapies like beta blockers and diuretics.

Bisphosphonates Inhibit Aneurysm Formation and Growth

UW–Madison researchers have developed methods for using bisphosphonate compounds to treat aneurysms.  After the researchers discovered robust calcification and osteoclast-like cells in the central layer of the aneurismal aorta wall in humans, as well as in an experimental abdominal aortic aneurysm model in mice, they hypothesized that overactivity of the osteoclast-like cells may induce the arterial damage that produces the aneurysm. By administering bisphosphonate, which inhibits osteoclasts, they showed complete inhibition of aneurysm formation in mice.