G-protein coupled receptors (GPCRs) are one of the most important molecules in medicine. Today, approximately one-third of drugs in the world work by targeting GPCRs. For a long duration, scientists have pondered whether GPCRs form heterodimers (consists of two different flavors of GPCR) or work alone. However, a conclusion yet to be reached due to the poor spatial resolution of current techniques. Earlier, several GPCRs have indeed been captured near each other in a cell, but it could not be assumed whether they were working together or not. The debate regarding receptor dimerization has only boiled fiercer with different labs providing different data through various methods.
A new imaging technique has been developed which might bring a stop to all these arguments. The method successfully captures movies of receptors on the living cell’s surface. It brings forth unprecedented clarity and could be a significant breakthrough for Medical Imaging Market as it could blaze the way for a trove of new innovative drugs. In the recent study, a research team zoomed in to the individual receptor proteins on the surface of cells to establish whether receptors work solo or come together to complete work.
GPCR heterodimers have great potential in the sector of pharmacotherapies, including disorders such as depression and schizophrenia. The team revealed that it was the chance to cause improvement in this field that drew them towards the current study. The new and powerful technique used herein was founded upon smFRET (Single-Molecule Fluorescence Resonance Energy Transfer). It helped researchers prove that dimers can be tracked as they move along the cell surface and the duration for which they last. This method uses the change that occurred in fluorescence when proteins (labeled with different fluorescent markers) are in extreme proximity. The resolution that arrives through this technique by the team is far greater (about ten times) than previous techniques.
The new method brings about several innovations in dyes, imaging, labeling technology, software, and protein engineering that enable tracking couples or individual receptors. In addition to detecting GPCR dimers, this approach also allows a clear view of how receptors change shape inside living cells once activated. The result is that researchers would now be better equipped to understand why and how drugs can impact the same receptors differently.
With the development of this method, further exploration can be held of receptor interactions and activation mechanizations with better resolution. This would provide the opportunity to discover new therapeutic approaches.
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