Articles tagged with G Protein Activation
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Researchers at Stanford University have developed a new synthetic receptor, PAGER, that can accommodate a broader range of inputs and produce a more diverse set of outputs. The tool enables control of neuronal activity, immune responses, and therapeutic treatments in lab experiments.
The study uses cryo-electron microscopy to observe the ETB receptor-G protein complex, revealing a strong binding interaction between G protein and ETB receptor. This finding may deepen understanding of endothelin signaling mechanisms and inform the development of new drugs.
The study elucidated the mechanisms behind G protein selectivity and efficacy in the human adenosine A2A receptor, discovering changes in activation conformations as the primary cause of coupling promiscuity. The research team used experimental and computational techniques to understand allosteric mechanisms and their role in selective...
Researchers propose targeting non-canonical HH/GLI signaling to improve response rate and durability of therapeutic effects exerted by SMO inhibition in melanoma. The findings suggest that combined targeting of hedgehog signaling and BRD4 could provide a novel therapeutic option against melanoma.
Scientists discovered a novel method to activate G protein-coupled receptors from inside cells, which can help develop drugs with fewer or no side effects. This new process uses a non-peptide message molecule called PCO371 that binds to the intracellular region of the receptor and interacts directly with G protein subunits.
Researchers at Johns Hopkins Medicine discover that nasal cell receptors activate few G protein molecules to produce a signal, contradicting the mainstream idea of high amplification. The study found that the probability of an odorant receptor activating just one G protein is 1 in 10,000, supporting weak signaling.
A Tel Aviv University study found a significant link between changes in G-protein-coupled receptors and brain adaptability. Disabling the voltage sensor of these proteins caused uncontrolled brain flexibility, leading to excessive habituation to odors.
Scientists challenge existing thinking on opioid tolerance and respiratory depression, proposing a new balanced approach to developing safer analgesics. They found that arrestin-3 engagement limits tolerance development but does not exacerbate respiratory depression.
A multinational team discovered at least two inactive and three active conformations of the human adenosine A2A receptor, dependent on ligands and G protein interactions. The study sheds new light on GPCR activation and signaling, offering opportunities for drug discovery.
Scientists from Johns Hopkins Medicine have challenged long-held assumptions about the processing of light in mammalian retinas. The study, published in Proceedings of the National Academy of Sciences, suggests that only 10-20 G protein molecules are activated by one rhodopsin molecule.
Researchers have created an artificial protein that inhibits G protein activators, leading to the potential blockage of malignant properties in cancer cells and correction of birth defects. The findings may pave the way for identifying new molecular targets for therapeutic intervention.
Researchers at Duke Health have discovered a new paradigm for how G protein-coupled receptors activate cell signaling mechanisms. The formation of 'mega-plexes' explains how signals can continue to be sent after internalization, opening up possibilities for targeted drug therapies.
Researchers created detailed fingerprints of G protein-coupled receptors, revealing complex interactions with signaling mediators. This breakthrough could lead to precise control of therapeutic effects and minimize adverse side effects.
Researchers have determined the complete three-dimensional atomic structure of an activated GPCR complexing with its G protein, shedding light on transmembrane signaling. The beta-2 adrenergic receptor's function was unknown despite being a key target for anti-asthma and blood pressure medications.
Researchers recreated a 240-million-year-old protein to study the vision of dinosaur ancestors, finding evidence that they may have had dim-light vision. The discovery offers insights into how biologically important molecules evolved over time and paves the way for further studies on ancient species.