Researchers Visualise Communication of G-protein Coupled Receptors

Study by IIT-Kanpur researchers published in the international journal Molecular Cell unravels a previously unknown mechanism that regulates an important class of drug targets known as G protein-coupled receptors

A group of researchers led by Prof Arun K Shukla in the Department of Biological Sciences and Bioengineering at the Indian Institute of Technology Kanpur (IIT-K) has unraveled a previously unknown mechanism that regulates an important class of drug targets known as G protein-coupled receptors. The discovery has important implications for not only understanding the fundamental mechanism of cellular signaling in our body but it also has potential to facilitate novel drug discovery for several human disease conditions. The study published in the May issue of the international journal, Molecular Cell has been conducted using a cutting-edge technology known as cryogenic-electron microscopy (cryo-EM).

The cells in our body are surrounded by a membrane that harbors a special type of protein molecules known as receptors. These receptors are important for our body to sense different chemical & hormones and respond accordingly by activating specific physiological responses. One particular class of receptors known as G protein-coupled receptors (GPCRs), is involved in regulating heart function, blood pressure, mental disorders, and our behavior. Several drugs such as those used for depression, heart failure, cancer and hypertension work by modulating these receptor proteins.

The function of GPCRs is regulated by another family of proteins in our body known as arrestins, which bind to GPCRs and control their function and physiological responses. However, a complete understanding of GPCR-arrestin interaction has been mostly elusive so far. The researchers have now visualised the cross-talk of GPCRs and arrestins in great detail using the cutting-edge technology, cryogenic-electron microscopy (cryo-EM). The same has allowed the team to discover a novel mechanism that is responsible for regulating the function of GPCRs in our body.

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