Articles tagged with G Protein Coupled Receptors
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Researchers from the University of Copenhagen have identified five new GPCRs activated by 17 peptide ligands, expanding the known peptide-GPCR network. This discovery has high translational potential as therapeutic targets for various diseases, including genetic, nervous system, and neoplastic disorders.
The study reveals the detailed 3D structure of the CysLT1 receptor, which plays a crucial role in inflammatory processes and allergic diseases like asthma. The researchers used advanced X-ray sources to determine the receptor's mechanism of operation, providing insights into improving asthma medications.
The study uncovered several hundred coupling events between GPCRs and G-proteins, greatly expanding the understanding of how these receptors work. This new data enables better prediction of GPCR-G-protein coupling and potential design of artificial GPCRs with specific signalling properties.
Researchers discovered a molecule involved in immune cell migration that plays a critical role in establishing immune responses. The COMMD3/8 complex promotes signal transduction of chemokine receptors to facilitate immune cell migration, which is essential for efficient immune responses and proper functioning of the immune system.
Researchers outline detailed sequence of events where a GPCR encounters its downstream signaling partner, providing insights into fundamental mechanisms of drug-induced signaling. The new analysis technique can identify precise amino acids most central to GPCR function, enabling potential sites for precision drug targeting.
A team of scientists has mapped a molecular complex that could aid in the development of better medications with fewer side effects for osteoporosis and cancer. The findings provide insight into how PTH1R interacts with key messengers to regulate calcium levels.
Researchers genetically engineered yeast cells to control their response to environment, improving our understanding of cell signaling. This breakthrough has immediate biotechnology uses and could lead to new treatments for diseases by modifying diseased cells.
Researchers at UC San Diego School of Medicine discovered that ubiquitination influences GPCR function and promotes inflammation. Existing cancer drugs targeting enzymes involved in ubiquitination may be repurposed to treat vascular inflammation.
Scientists at the University of Würzburg have developed a new method called BRET that allows them to test the activity and potency of G protein-coupled receptor (GPCR) ligands in living cells. This breakthrough enables faster discovery of novel pharmaceutical substances with less side effects.
Researchers discovered a llama-derived nanobody that specifically targets G beta-gamma signaling, preventing it from activating several other signaling proteins. This approach may provide control over multiple GPCRs and avoid undesired cellular events.
Researchers discovered that activating GPR139 reduces alcohol intake and restores pain sensitivity thresholds in alcohol-dependent mice. This finding suggests a potential new approach for treating alcohol use disorder.
Scientists have visualized the interaction between two critical components of the body's cellular communication network using cryo-electron microscopy. The near-atomic resolution images show a G-protein coupled receptor bound to an inhibitory G protein, providing a blueprint for designing more precise and selective drugs.
Scientists at Charité and Stanford University decipher the molecular step of cellular signal transmission involving G protein-coupled receptors (GPCRs) and arrestin. The study's findings could lead to the development of specific drugs targeting diseases like asthma, schizophrenia, hypertension, and cancer.
A multi-institutional project has provided new understanding of how GPCRs regulate in response to physiological ions like sodium, calcium, and magnesium. This research could lead to more effective drugs for controlling pain, hunger, and other conditions by targeting the receptors' function.
Scientists at NIDA uncovered evidence of a more complex role for GPCRs, suggesting a conceptual advance in biochemistry and pharmacology. The discovery reveals that GPCRs form part of pre-coupled macromolecular complexes that act as computing devices to gather and process information.
A recent study by Johns Hopkins researchers found previously known skin itch receptors in the airways of mice, which appear to contribute to bronchoconstriction and airway hypersensitivity. The discovery may be a promising new target for developing drug therapies for asthma and other respiratory disorders.
Scientists at SIMM have determined the crystal structure of the human glucagon receptor in complex with a glucagon analogue, providing insights into its activation mechanism. The study reveals significant conformational changes in the linker region and extracellular loop that facilitate peptide binding and initiate receptor activation.
Researchers at Scripps Research Institute use nuclear magnetic resonance spectroscopy to study the A2a adenosine receptor, revealing its dynamic structure and a
Researchers mapped genetic mutations in GPCRs and found that 3% of population have receptors with altered drug effects. The study estimates an economic burden of at least 14 million pounds annually on the UK National Health Service.
Scientists identified a compound, FR, that provides long-lasting airway relaxation and prevents hyperreactivity in mouse models of asthma. The locally administered compound also blocks aspects of airway remodeling without causing cardiovascular side effects.
Researchers have discovered that G protein-coupled receptors (GPCRs) are active in the cell interior, influencing gene transcription and cell division. This finding has implications for developing innovative drugs targeting receptor function or uptake.
Researchers discover latrophilin/CIRL receptor's mechanism of action, using ion channels and intracellular messengers to trigger signal cascades. The study uses Drosophila larvae and super-resolution microscopy to visualize receptor location and signal transmission.
Researchers reveal components of rhodopsin and arrestin that form a critical cellular communication network. The discovery provides new insights into how GPCRs interact with signaling molecules, potentially leading to more effective drugs with fewer side effects for diseases like heart failure and cancer.
Researchers captured the first cryo-electron microscopy snapshots of a key cellular receptor in action, providing near-atomic-resolution images. The study reveals how peptide hormones like GLP-1 bind to and transmit signals through G protein-coupled receptors.
Researchers have made significant progress in understanding the structure of the glucagon receptor, a key component in glucose regulation. The study provides detailed molecular information that can guide the development of more accurate and efficient diabetes drugs.
Researchers have developed a new technique that allows for precise mapping of cellular signaling networks involved in human biology and disease. This breakthrough opens up exciting avenues for understanding and treating psychiatric diseases, including opioid addiction.
USC scientists discovered unexpected characteristics of the AT2 protein, which interacts with the angiotensin II hormone regulating blood pressure. The study reveals potential new paths to drugs controlling cardiovascular disease and pain, offering an important first step towards targeted therapies.
Researchers have discovered new structural details of the angiotensin II receptor AT2R using X-ray free electron laser technology. The findings could speed the development of new compounds addressing cardiovascular conditions, neuropathic pain and tissue growth.
Researchers have found that cholesterol can regulate the activity of the adenosine receptor by accessing its active site, potentially leading to new treatments for diseases such as Alzheimer's. This discovery could also have implications for other central nervous system diseases where GPCRs play a key role.
The study reveals that arrestin's C-edge loops interact directly with the membrane, forming a new type of binding. This discovery opens up new avenues for understanding the role of the membrane in GPCR-arrestin interactions and developing drugs with fewer side effects.
Researchers are studying how receptors are transported from inside the cell to the surface where they function. Small proteins like Rab43 play a crucial role in this process, helping to ensure the proper functioning of GPCRs.
Researchers at FAU discovered that cholesterol strongly influences CXCR4 dimerization and signal transmission in human cells. Their computer simulations revealed that cholesterol is required for the correct formation of GPCR pairs, which affects their function.
A new study reveals that cholesterol selectively binds to specific regions of GPCR proteins, enabling them to form paired structures and sense external signals. This discovery could open up new avenues for drug discovery and understanding cancer metastasis and AIDS.
An international team of scientists has created a three-dimensional atomic-level image of the human cannabinoid receptor 1 (CB1), revealing an expansive and complicated binding pocket network. The findings have potential to guide drug design for pain, inflammation, obesity, fibrosis, and other indications.
A research team from UC San Diego and Monash University identified 38 lead compounds that exhibit strong affinity and high selectivity for the M2 mAChR binding site. These compounds target allosteric binding sites, which are built around a more diverse genetic sequence and structure than orthosteric binding sites.
Researchers at TUM have determined the mechanism of G protein switching, providing insights into the design of new active agents. The study reveals that the open form of the protein is more accessible to active agents than its rigid, closed form.
Researchers have identified a new therapeutic approach to prevent renal damage in cardiorenal syndrome type 2 (CRS2), a condition that causes chronic kidney disease secondary to heart failure. By inhibiting G protein-coupled receptors, the study found that renal function can be protected.
Temple researchers have uncovered a new mechanism by which aldosterone triggers heart damage, involving GRK2 and GRK5 signaling molecules. The study found that inhibiting these kinases could provide a potential therapeutic solution for heart failure.
Researchers at TSRI have discovered the dynamics of β2 adrenergic receptor (β2AR), a protein linked to asthma, obesity and type 2 diabetes. The study found that β2AR naturally fluctuates between its active and inactive states in the absence of any drug, and different drugs can either stimulate or inhibit signaling.
The Scripps Research Institute (TSRI) team has discovered a unique anti-diabetes compound that activates the GLP-1 receptor's G-protein pathway, potentially leading to a new type of diabetes treatment. The novel molecule P5 shows promise in boosting glucose tolerance with minimal insulin stimulation.
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.
A new high-resolution method allows precise identification and quantification of interactions between a receptor and two ligands. Scientists have developed a novel approach using atomic force microscopy, enabling the imaging of single membrane receptors while detecting their interactions with multiple ligands.
Dr. Lefkowitz's research reveals that all GPCRs share the same structure, enabling the development of more effective and safer drugs for various pathologies including type 2 diabetes and obesity.
Early-career cell biologists Clifford Brangwynne, Ahmet Yildiz, and Meng Wang have won the ASCB-Gibco Emerging Leaders Prizes for their groundbreaking research in cell biology. Their work has launched new research fields at the interface of biology and physics.
Researchers found that Ebola and Marburg viruses use G protein-coupled receptors to enter cells, which can be blocked by existing drugs targeting these receptors. The study identified 20 GPCR antagonists effective against the two viruses, paving the way for potential therapeutics.
Researchers used X-ray crystallography to visualize the structure of a neurotensin receptor, shedding light on its mechanism. Binding of neurotensin to the receptor triggers critical conformational changes that activate G protein-coupled signaling pathways.
A new study has provided never-before-seen details of the human body's cellular switchboard that regulates sensory and hormonal responses. The research, led by Eric Xu at the Van Andel Research Institute, used SLAC's X-ray laser to complete the first 3-D atomic-scale map of a key signaling protein called arrestin.
Researchers used a powerful X-ray laser to create a three-dimensional map of a key protein complex, revealing its structure and interactions. This breakthrough provides insights into developing more targeted therapies for diseases like cancer and heart disease.
Researchers at Vanderbilt University have discovered a novel cell signaling pathway that may provide new insights into obesity. The discovery centers on the melanocortin-4 receptor, which plays a key role in regulating appetite, and reveals a molecular mechanism for converting an on-off switch into a rheostat.
A researcher at American University has constructed a three-dimensional computer model of a receptor protein linked to human growth, which may lead to the development of drugs to treat conditions such as gigantism and dwarfism. The study was led by researchers from the Eunice Kennedy Shriver National Institute of Child Health & Human D...
Scientists used computer modeling to trace water channels in cell surface receptors (GPCRs), discovering their role in signal transduction. The study suggests that targeting these internal water pathways could lead to the development of more efficient drugs.
Researchers at Duke University, University of Michigan, and Stanford University have determined the underlying architecture of a cellular signaling complex involved in responding to stimuli such as light and pain. The findings reveal a two-step mechanism that has been hypothesized previously but not directly documented.
Researchers at Monash University developed a new class of drug targeting alternative recognition sites on GPCRs to fine-tune protein behavior, reducing damage and potential side effects. The breakthrough could lead to the creation of a new treatment for heart attacks and heart failure.
Researchers at Scripps Research Institute and Vanderbilt University have created the most detailed 3-D picture yet of a membrane protein linked to learning, memory, anxiety, pain and brain disorders. The study focused on the mGlu1 receptor, which helps regulate neurotransmitter glutamate.
Scientists at LMU developed photoreactive compounds that modulate nerve-cell function, opening new routes to treat neurological diseases like chronic pain and visual impairment. They created hybrid photoreceptors that respond to light, potentially leading to new therapies for these conditions.
Researchers at Scripps Research Institute have developed a new method to map the 3D structure of membrane proteins, including the human serotonin receptor. This approach enables faster and more accurate imaging, potentially condensing the timeline for structural studies from months to days.
ASU researchers have successfully imaged G-protein-coupled receptors at room temperature using serial femtosecond crystallography. The new method allows for the study of human proteins without freezing, reducing radiation damage and enabling the observation of molecular dynamics.
Researchers used X-ray laser to map the 3D structure of a key cellular gatekeeper, the human serotonin receptor. The breakthrough technique uses smaller crystals and produces high-resolution images, potentially condensing years-long studies into days.
Researchers at Stanford and Google have successfully simulated the transformation of a key drug receptor site using Google Exacycle's cloud computing platform. The simulation revealed thousands of possible configurations, providing scientists with a better jumping-off point for computational drug design.
Researchers at Monash University have combined computer modelling with pharmacology to gain new insights into how the body interacts with novel drug treatments. The study reveals alternative drug recognition sites on G protein-coupled receptors, which play a role in virtually every biological process and most diseases.