A new protein finding likely to pave way to better heart therapies

 group of scientists found surprising features of an enigmatic protein. This might enable to uncover many new paths to drugs for a variety of chronic illness.

According to the study, published online in the journal Nature, scientists have uncovered peculiar characteristics of a key protein, which is linked to blood pressure control and to nerve growth, pain control and heart tissue regeneration. The protein is called AT2, and it is one of a group of receptors that interact with the angiotensin-II hormone, which regulates blood pressure. Angiotensin II receptor proteins are important factors in diabetes, hypertension, heart attack and congestive heart failure, and stroke. The findings likely are likely to open doors to potential new therapies to control cardiovascular disease and pain.

According to Cherezov and Vsevolod Katritch, researchers involved in the study,  AT2 is a member of a super family of proteins called G protein-coupled receptors, or GPCRs. These receptor proteins span the cell membrane, responding to different stimuli outside the cell - nutrients, hormones and even light - then triggering responses inside the cell.  Because they are active in so many physiological processes in both healthy and disease states, GPCRs like AT2 are important drug targets.

"AT2's activity has been observed on the organ and organism level, but how it works on the molecular level is not understood," said researcher Vadim Cherezov.

That's in part because AT2 doesn't behave like other GPCRs, "AT2 does not work through canonical signalling pathways for GPCRs.It doesn't activate a G protein and it doesn't work through arrestins, added Katritch.
In most cases, G proteins and a group of proteins called arrestins interact with a cleft that opens up on the intracellular side of GPCRs upon activation. When a stimulus triggers the GPCR from outside the cell, the GPCR activates a G protein or arrestin within the cell, which then relays the signal to other proteins in the cell, and so on, in something akin to a game of molecular called telephone.

Cherezov, while noting that further research is very much needed, concludes that the current discovery is an important first step both to better understanding of similar atypical GPCRs and to potential new therapies.

News Source: ANI

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