G-protein-coupled receptors (GPCRs) present in the body are acts as signal transducers which allows cells to respond to their external environments. GPCRs play a crucial role in numerous biological functions such as heart rate, vision, smell, and taste allergic responses. GPCR malfunction might lead to a rising in the number of diseases and side effects many therapeutic drugs works due to its influence on these proteins.
Researchers at the University Of California San Diego School Of Medicine have new ways to use the GPCRs and their cellular waste disposal systems to control inflammation. The findings were published in the Cell Reports on 18 September, which suggested some existing cancer drugs that inhibit these cellular activities to treat vascular inflammation, which occurs when artery-blocking plaques formed in atherosclerosis.
Senior author of the study JoAnn Trejo, Ph.D., professor in the Department of Pharmacology and dean of faculty affairs at UC San Diego School of Medicine said that they observed the GPCRs and inflammation influenced by the ubiquitination. Ubiquitination is a process was previously used for the marking the proteins for destruction. Now the both GPCR and ubiquitination are used.
When the molecules of nutrients, connected to GPCR on the outside of the cell, the GPCR changes shape. While on the other side of the membrane the G-protein docks are newly repositioned GPCR. Based on the type of signal and cell, the G-protein then removes the cascade of molecular events.
According to Trejo, a handful of drugs that inhibit E3 ubiquitin ligases are approved by the Food and Drug Administration (FDA) for effective treatment of some of the types cancer such as myeloma, mantle cell lymphoma, and others.