Researchers have shown that the regulation of G Protein-Coupled Receptors (GPCRs) by new drugs can be simpler than generally thought — it can be mediated by engaging only the end of the receptor, which is called the tail of the receptor.
How GPCRs Operate?
- The part of the receptor that protrudes outside the membrane changes its shape whenever a stimulus in the body binds to it. In response to this change in the outside part of the receptor, a corresponding change happens in the shape of the receptor that is positioned inside the cell.
- This change in the shape of the receptor positioned inside the cell allows it bind to other proteins called effectors. These effectors cause specific effects in the cell, referred to as cell signalling, which leads to physiological changes in our body.
- Through specific engineering of the receptor researchers basically disrupted one of the two binding sites, namely the core of receptor. They found that even without the second site, the protein was able to pull the receptor inside the cell by binding just to the tail of the receptor.
- There is a key region in the core which the researchers genetically deleted thereby making the core of the receptor ineffective.