Search Results
118 items found for "Nicolas Jaime Roth"
- PAR-Induced Harnessing of EZH2 to β-Catenin: Implications for Colorectal Cancer
Both PAR4 and PAR2 are able to drive the association of methyltransferase EZH2 with β-catenin, culminating
- Combined docking and machine learning identify key molecular determinants of ligand pharmacological
Meanwhile, the antagonist ligands made interactions with W2866.48×48 and Y3167.43×42, both residues considered
- Glyco-sulfo hotspots in the chemokine receptor system
sites of N-acetyl galactosamine (GalNAc)-type O-glycosylation in their N-termini as well as sulfation, both Both PTMs were shown to contribute to the binding of CCL5 and CCL8 and to a minor extend CCL3. The combined effects of both PTMs as well as the relevance of specific acceptor sites and glycan composition
- Adrenal G Protein-Coupled Receptors and the Failing Heart: A Long-distance, Yet Intimate Affair
Chronic human HF is characterized by several important neurohormonal perturbations, emanating from both
- Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and...
Pharmacological targeting of cGAS/STING-YAP signaling by both a small-molecule STING agonist, SR-717,
- GRK2 in cardiovascular disease and its potential as a therapeutic target
interactome includes numerous proteins which interact with differential domains of GRK2 to modulate both
- Engineered synaptic tools reveal localized cAMP signaling in synapse assembly
In vivo, suppression of postsynaptic cAMP signaling in CA1 neurons prevented formation of both Schaffer-collateral
- Signaling pathways activated by sea bass gonadotropin-inhibitory hormone peptides in COS-7 cells...
evident increase in SRE-luc activity was noticed when COS-7 cells expressing GnIHR were challenged with both
- Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on Inflammation..
Here, we report that the Ovarian Cancer G-Protein Coupled Receptor1 (OGR1 or GPR68) has dual roles in both
- Exploiting Dependence of Castration-Resistant Prostate Cancer on the Arginine Vasopressin ...
In CRPC xenografts, antagonizing AVPR2, AVPR1A, or both significantly reduced CRPC tumor growth as well
- A Model for the Signal Initiation Complex Between Arrestin-3 and the Src Family Kinase Fgr
reports demonstrated that Fgr exhibits high constitutive activity, but can be further activated by both
- Allosteric ligands control the activation of a class C GPCR heterodimer by acting at the transmembra
The data support the inference that they act at the active interface between both transmembrane domains
- GPR3 expression in retinal ganglion cells contributes to neuron survival and accelerates axonal...
Our earlier reports suggested that GPR3 enhances both neurite outgrowth and neuronal survival.
- Structural landscape of the Chemokine Receptor system
the N-loop determines the subfamily-specific arrangement of the distal N-terminus and the 30s-loop, both By examining both the active and inactive states of CCR5, it becomes evident that there are four distinct Constitutive Activity of the viral CKR US28 and “Chemokine Scavenger” ACKR3 Both US28 and ACKR3 are constitutively Experimental 3D structures of both receptors reveal that they employ distinct mechanisms for constitutive
- On-cell nuclear magnetic resonance spectroscopy to probe cell surface interactions
In this review, we outline some key NMR techniques applied for on-cell NMR studies through both solution
- New role of β-arrestins in MOR signaling
At the synapse, they are localized in both pre- and postsynaptic compartments and their activation is The authors found that both β-arrestin 1 and 2 are involved in MOR internalization and downstream signaling
- GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between ...
however, attention has focused upon how stable multiprotein GPCR superstructures, termed receptorsomes, both
- Targeting Intracellular Allosteric Sites in GPCRs
influence the orthosteric binding pocket, potentially altering the rate of association, dissociation, or both On the other hand, selectivity could be achieved by merging both orthosteric and allosteric pharmacophores
- Free-Energy Simulations Support a Lipophilic Binding Route for Melatonin Receptors
simulations which revealed different trajectories passing through the gap between TM helices IV and V for both
- Characterization of a new WHIM syndrome mutant reveals mechanistic differences in regulation of ...
In contrast to wild type CXCR4, both R334X and S339fs5 were largely insensitive to CXCL12-promoted degradation
- Melatonin MT 2 receptor is expressed and potentiates contraction in human airway smooth muscle
mediated via its specific G protein-coupled receptors (GPCRs) named the MT1 receptor, which couples to both
- Involvement of various chemokine/chemokine receptor axes in trafficking and oriented locomotion ...
chemokine receptor axes play a pivotal role in the recruitment and oriented trafficking of immune cells both
- Unlocking the Therapeutic Potential of Previously Undruggable GPCRs
activation of cytosolic effector proteins: the G proteins after which GPCRs are named, and arrestins which both points of contact it is possible not only to strongly increase binding affinity but also to fine tune both transmembrane domain providing significantly increased binding affinity and providing a means to control both Both properties enable enhanced ligands to avoid being eliminated during the stringent washing process at killing cells than unconjugated MMAE, the Orion CCL5 superagonist analog significantly increased both
- Dynamic GPCR activation revealed through time-resolved Cryo-EM
the movement of Switch II towards the nucleotide-binding pocket and the stabilization of Switch III, both
- Neuronal Gα subunits required for the control of response to polystyrene nanoparticles in the ...
required for the control of response to polystyrene nanoparticles in the range of μg/L in C. elegans The aim Caenorhabditis elegans was used as an animal model, and both gene expression and functional analysis
- 📰 GPCR Buzz: August 5-11, 2024 | Top Highlights from DrGPCR University!
Check out what’s coming in September and October: Sign up for both courses now and score a 25% early
- 📰 GPCR Weekly News, August 28 to September 3, 2023
stimulates human ovarian cancer cell invasion by upregulating MMP-9 via ERK1/2 signaling CCR7 acts as both
- Biased Agonism at the GLP-1 Receptor: A Pathway to Improved Therapeutic Outcomes
diabetic models have shown that although exendin-P5 induces lower insulin release compared to exendin, both