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Results found for "drug discovery"
- Activation of the human chemokine receptor CX3CR1 regulated by cholesterol
However, the drug development of CX3CR1 is hampered partially by the lack of structural information.
- TM5-TM6: structural switches that modulate the coupling of serotonin receptors to Gs or Gi
The discovery of the orthosteric binding pocket is of great importance in GPCRs field as it supports the development of alternatives to improve drug design to optimize receptor selectivity.
- Integrative model of the FSH receptor reveals the structural role of the flexible hinge region
The models are expected to allow for testable hypotheses about signal transduction and drug development
- Molecular insights into regulation of constitutive activity by RNA editing 5HT2C serotonin receptor
5HT2C-transducer-coupled structures of three representative isoforms (INI, VGV, and VSV) with the selective drug
- Hear the sounds: the role of G protein-coupled receptors in the cochlea
And A1, A2A, and CB2 activation by agonists has protective functions on noise- or drug-induced hearing
- 📰 GPCR Weekly News, May 1 to 7, 2023
GPCR Binders, Drugs, and more Adenylyl cyclase 6 plays a minor role in the mouse inner ear and retina Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.
- Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of ligand...
To understand the basis of the ligand preferences of the receptors and to assist structure-based drug
- Location bias contributes to functionally selective responses of biased CXCR3 agonists
is critical to the overall biased response observed at CXCR3, which has important implications for drugs
- Search for safer pain relief advances with new engineered compounds
in Florida have created a collection of new pain-relieving compounds that, like morphine and other drugs
- Nanobodies as Probes and Modulators of Cardiovascular G Protein-Coupled Receptors
cardiovascular medicine due to the critical physiological roles of these receptors and their prominence as drug
- Fluorescent Ligands Targeting Intracellular Allosteric Binding Site of the Chemokine Receptor CCR2
binding site (IABS) of the CC chemokine receptor 2 (CCR2), a class A GPCR that has been pursued as a drug
- Constitutive, Basal, and β-Alanine-Mediated Activation of the Human Mas-Related G Protein-Coupled ..
expressed in mast cells, macrophages, and in cardiovascular tissue, linking them to pseudo-allergic drug mediator and supports the notion that IL-6 can be used as a marker for MRGPRD activation in an in vitro drug
- G-protein-coupled receptors as therapeutic targets for glioblastoma
receptor-4 (MC4R), adhesion, lysophosphatidic acid (LPA) and smoothened (Smo) receptors to initiate new drug-screening
- Functional modulation of PTH1R activation and signaling by RAMP2
of a GPCR that may provide a new venue for highly specific modulation of GPCR function and advanced drug
- Ligands can differentially and temporally modulate GPCR interaction with 14-3-3 isoforms
certain GPCR ligands can regulate GPCR/14-3-3 signals temporally, suggesting a new approach for GPCR drug
- Case Report of a Juvenile Patient with Autism Spectrum Disorder with a Novel Combination of Copy...
under methylphenidate treatment but responded positively to 3 mg per day of the atypical neuroleptic drug
- Cholesterol-Dependent Dynamics of the Serotonin 1A Receptor Utilizing Single Particle Tracking....
signaling hubs in cell membranes that regulate a wide range of physiological processes and are popular drug
- Cholesterol-Dependent Dynamics of the Serotonin1A Receptor Utilizing Single Particle Tracking: ...
signaling hubs in cell membranes that regulate a wide range of physiological processes and are popular drug
- Mechanistic Understanding of the Palmitoylation of Go Protein in the Allosteric Regulation of...
regulation of aGPCRs via post-translational modifications of the Go protein, and offers guidance for future drug
- Novel Therapies for Cardiometabolic Disease: Recent Findings in Studies with Hormone...
findings regarding the complex biology of the preproglucagon-derived hormones, their signaling, and the drug
- APEX2/AUR Biosensor: A Powerful Tool for Protein Interaction and Trafficking
development of molecular tools to study GPCR trafficking in real-time opens new avenues for understanding drug
- GPR84 signaling promotes intestinal mucosal inflammation via enhancing NLRP3 inflammasome activation
in innate immune cells and intestinal inflammation, and suggest that GPR84 may serve as a potential drug
- Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal...
implications in structural biological advancements of GPCRs and design of thermally stabilized receptors for drug
- In vitro assays for the functional characterization of (psychedelic) substances at the serotonin...
Besides their appearance on the (illicit) drug market, e.g. as new psychoactive substances, their potential
- A2B Adenosine Receptor Enhances Chemoresistance of Glioblastoma Stem-Like Cells under Hypoxia: New..
chemoresistance of GSCs is mediated in part by adenosine signaling and ABC transporters, which extrude drugs
- G protein-coupled receptors that influence lifespan of human and animal models
We also discuss the possibility of using agonist or antagonist drugs, depending on the beneficial or
- Intermolecular Interactions in G Protein-Coupled Receptor Allosteric Sites at the Membrane Interface
Calculations "Allosteric modulators are called promising candidates in G protein-coupled receptor (GPCR) drug
- GRK2 in cardiovascular disease and its potential as a therapeutic target
These data support the premise that GRK2 should be at the forefront of a novel investigative drug search
- G protein-biased GPR3 signaling ameliorates amyloid pathology in a preclinical Alzheimer's disease..
preferentially activate G protein or β-arrestin signaling pathways, are leading to the development of drugs
- Increased Anxiety-like Behaviors in Adgra1-/- Male But Not Female Mice are Attributable to...
pathways in amygdalae of male mice, implicating a potential, therapeutic application in novel anti-anxiety drug
