Pharma Focus Asia
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New Approach to Manipulating GPCRs

G-protein-coupled receptors or GPCRs are the most important signalling mechanism in human cells. They react on exposure to the nutrients, toxins, hormones and light particles. The major blockbuster drugs target the GPCRs for treatment of many diseases including heart disease, cancer, diabetes, depression and arthritis. These drugs affect GPCRs behaviour external to the cells. Research scientists have devised a way to manipulate the GPCRs to influence signalling on the inside of cells.

The Study of G-Proteins has been going on since 1994. In the early findings, scientists discovered a flexible “hotspot” where major interactions of enzymes take place with the GPCRs. The current research included a computer simulated experiment to find out which drug-like molecules would bind tightly to the hotspot from an existing database of 1990 known structures as well as ranking them.

Researchers have found that two compounds - M119 and M201 were most effectively bound to the hotspot. Use of M119 resulted in reduced enzyme activation that caused inflammation. M201 involved pain relief brought about by morphine.

The research team at University of Rochester believes that identification of 50 small molecules, brings about a specific set of changes in the behaviour of the hotspot. This would give precise control over one of the most important biochemical switches in the body. The study has implications towards drugs becoming more effective and a novel method of treating the diseases.

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