10 February 2014

Reducing "bad" cholesterol: another promising method

A new approach to the treatment of atherosclerosis has been found

Copper news based on the materials of Science Daily: A new way for reducing 'bad' cholesterol?The data obtained by Danish scientists can open a new chapter in the treatment of atherosclerosis and enable the pharmaceutical industry to develop a new, effective drug to reduce the so-called "bad" cholesterol, which is the cause of the development of cardiovascular diseases – the "number one killer" in the world.

The results of this work are published in the journal Cell Metabolism (Gustafsen et al., The Hypercholesterolemia-Risk Gene SORT1 Facilitates PCSK9 Secrecy).

About ten years ago, it was discovered that the level of "bad" cholesterol can be reduced by inhibiting the enzyme PCSK9 (proprotein convertase subtilisin-kexin type 9), mainly synthesized in the liver. It has been established that this secretory protein is able to have a destructive effect on the receptors of liver cells, which is why they lose the ability to bind and remove low-density lipoproteins (LDL) from the blood. The development of drugs based on antibodies blocking the PCSK9 enzyme has already become a new hope in the treatment of atherosclerosis, and the first clinically tested drugs of this kind are likely to be approved this year.

However, the new study has taken a step further. In the course of studying the nature and functions of the PCSK9 enzyme, a research team from Aarhus University discovered an important element in the mechanism of its operation - a specific cell receptor sortilin, which has a decisive influence on the activity of this protein.

As it turned out, sortilin increases the activity of the PCSK9 protein, so if this receptor is inhibited, it will cause a drop in enzyme activity and, as a result, lead to a decrease in LDL levels in the blood. According to scientists, this approach, the target of which is this system of cellular receptors, opens up new opportunities in the treatment of elevated cholesterol levels.


Diagram from an article in Cell Metabolism – VM

The positive effect of sortilin suppression has been shown by scientists in experiments on mice, and now they plan to start clinical trials. In the future, researchers hope to create a drug that can be a good alternative to statins. Currently, statins are actively used all over the world to reduce "bad" cholesterol, but they have some contraindications and undesirable side effects.

"For the last ten years, all attention has been focused on PCSK9," Science Daily quoted one of the authors of the study, Simon Glerup, as saying. "Now we present a new discovery that accompanies a greater understanding of PCSK9 and may, at the same time, open the way to a new strategy in the treatment of atherosclerosis that has the same effect as PCSK9 inhibitors."

According to him, the possibility of selling a drug based on PCSK9 enzyme inhibitors in the future is already protected by patent and property rights, while a new approach to the treatment of patients suffering from atherosclerosis may provide other pharmaceutical companies with the opportunity to develop a completely new drug.

Portal "Eternal youth" http://vechnayamolodost.ru10.02.2014

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