Search Results
268 items found for "drug combination"
- 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
- Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based kinet
Nevertheless, the GloSensor™ cAMP assay can be applied to analyze signaling by a wide range of GPCRs for drug
- 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
- Differences across sexes on head-twitch behavior and 5-HT2A receptor signaling in C57BL/6J mice
of DOI differed among sexes - brain and plasma concentrations of DOI were lower 30 and 60 min after drug
- 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
- 📰 GPCR Weekly News, April 8 to 14, 2024
peptide-induced relaxation of human coronary arteries: A key role for Gβγ subunit instead of cAMP GPCR Binders, Drugs next-generation medicines G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug
- Chemogenetic stimulation of the G i pathway in astrocytes suppresses neuroinflammation
(GPCRs) are commonly used in chemogenetics as designer receptors exclusively activated by designer drugs
- 📰 GPCR Weekly News, May 6 to 12, 2024
receptors supports the independent expansion of bilaterian and cnidarian peptidergic systems GPCR Binders, Drugs 1117-2520: A Potent and Selective Antagonist of CCR6 for Autoimmune Diseases MRGPRX4 mediates phospho-drug-associated
- Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β-Arrestin ...
These receptors are the most clinically productive drug targets at present.
- Allosteric Effect of Nanobody Binding on Ligand-Specific Active States of the β2 Adrenergic Receptor
binding partners on the GPCR activation mechanism, which should be taken into account in structure-based drug
- Deficiency of β-arrestin2 alleviates apoptosis through GRP78-ATF6-CHOP signaling pathway in ...
syndrome The etiology of primary Sjögren's syndrome (pSS) remains unknown, and there is no ideal drug
- Self-docking and cross-docking simulations of G protein-coupled receptor-ligand complexes
Ligand discovery aimed at identification of chemical tools and drug leads is aided by molecular docking
- An overview of the compartmentalized GPCR Signaling: Relevance and Implications
Drug discovery today, 24(11), 2192–2201. https://doi.org/10.1016/j.drudis.2019.09.003 Ferrandon, S., Functional selectivity of GPCR-directed drug action through location bias.
- Unveiling GPCR Priming: The Hidden Synergy in Cellular Signalling
This has significant implications for drug development, as targeting these non-cognate interactions could
- 📰 GPCR Weekly News, July 17 to July 23, 2023
MPGPCR Conference (November 15 -17, 2023) Structure, Mechanism, and Drug Interactions of GPCRs, Ion Channels
- Nanobodies: New Dimensions in GPCR Signaling Research
lightly represent the potential applications of Nbs to facilitate the development of more selective drugs Combinatorial biology methods such as phage display, yeast display, and ribosome display can be used
- Therapeutic validation of an orphan G protein‐coupled receptor
better tools to study its function in both disease and physiological settings will likely potentiate drug
- 📰 GPCR Weekly News, April 22 to 28, 2024
thereof Ubiquitin-driven G Protein-Coupled Receptor Inflammatory Signaling at the Endosome GPCR Binders, Drugs
- Jan Steyaert Named 2022 Jacob and Louise Gabbay Award Winner
This award recognizes the combination of Steyaert’s fundamental research and his ability to apply the sciences with the mechanistic understanding of one of the biggest classes of pharmaceutical targets by combining
- Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer Cells...
Here, we show that a combination of insulin and the GPCR agonist neurotensin induced rapid activation A combination of dasatinib and trametinib potently and synergistically inhibited colony formation by The results provide rationale for considering a combination(s) of FDA-approved SFK (dasatinib) and MEK
- Although the cannabinoid type-2 receptor (CB2) is highly expressed in the immune system, emerging...
Recent anatomical studies, combined with electrophysiological studies, indicate that CB2 receptors are The ability of CB2 receptors to inhibit dopaminergic and hippocampal circuits, combined with the anti-inflammatory
- 🎧Episode 85 of the Dr. GPCR podcast is here!
Nicholas Holliday and how he has combined his university role with his leadership of Excellerate Bioscience
- Overview of adhesion GPCRs self-activation
Indeed, despite their broad physiological importance in normal and pathological processes, so far no drugs
- Feeder or trigger – CCR2 as a scavenger and regulator of cell migration
What are the implications in drug discovery?
- Dr. Rosie Dawaliby Podcast!
🥁 Drum rolls, please! Our guest is the wonderful Dr. Rosie Dawaliby!
- Structural view of G protein-coupled receptor signaling in the retinal rod outer segment
We have combined recently published cryo-electron tomography (cryo-ET) data on the ROS with structural
- Endogenous ligand recognition and structural transition of a human PTH receptor
Furthermore, five distinct PTH-bound structures, combined with computational analyses, provide insights