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Results found for "Bryan L Roth"
- Discovery of 3(2-aminoethyl)-thiazolidine-2,4-diones as a novel chemotype of sigma-1 receptor ligand
We have explored hydrophobic groups of different sizes on both sides of the five-membered ring scaffold
- Neuropeptide S Encodes Stimulus Salience in the Paraventricular Thalamus
Taking advantage of a striking deficit of both NPS receptor (NPSR1) and NPS precursor knockout mice in
- To probe the activation mechanism of the Delta opioid receptor by an agonist ADL5859 started from...
Although the high-resolution crystal structures of the DOR with both agonist and antagonist have recently
- GPR84 signaling promotes intestinal mucosal inflammation via enhancing NLRP3 inflammasome activation
Infiltrating GPR84+ macrophages are significantly increased in the colonic mucosa of both the UC patients
- Enzyme Inhibition Pharmacology: The Hidden Gatekeepers of GPCR Drug Discovery
Kenakin dissects how P450s can be both protective and problematic. Each mode reshapes both potency and therapeutic window.
- 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
- Structural basis of adhesion GPCR GPR110 activation by stalk peptide and G-proteins coupling
This is also where Gq/Gs bind the receptor through both hydrophobic and polar interaction, while Gi/G12
- Bell-Evans model and steered molecular dynamics in uncovering the dissociation kinetics of ligands..
In the experiment, similar sets of residues were found to be in significant contact with both ligands
- Anosmin 1 N-terminal domains modulate prokineticin receptor 2 activation by prokineticin 2
domain 1 (FnIII.1) suggest the cysteine-rich (CR) and the FnIII.1 domains could assist the WAP domain both
- In vitro assays for the functional characterization of (psychedelic) substances at the serotonin...
discussed that one should consider when attempting to compare functional outcomes from different studies, both
- 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
- 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
- TeachOpenCADD - A teaching platform for computer-aided drug design
Since we cover both the theoretical as well as practical aspect of these topics, the platform addresses
- Orthosteric vs Allosteric Interactions— and the pHSense Shift in Internalization
By carefully tuning both brightness and fluorescence lifetime, they engineered a two-dimensional pH response receptor localization and real-time signaling shape therapeutic outcomes, fluorescent ligands deliver both
- 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
- 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
- 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
- From GPCR Data Chaos to Decisive Action
Not possible when nothing’s built to surface the right insights early.
- 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
- 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.
- 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
- 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
- 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
- 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
- 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



