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Results found for "Dr. Bryan Roth"
- 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
- 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
- Using Live-cell High-Content Screening to Characterize CB2 Ligands: Insights From 16 Synthetic Cannabinoids
This dataset highlights how HCS can be used both to triage compound series and to extract quantitative signaling, tools that preserve cellular context will be increasingly important for designing ligands with both
- 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
- 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
- Differential binding of Δ9-tetrahydrocannabinol derivatives to type 1 cannabinoid receptors (CB1)
validity as a fluorescent probe for Tag-lite® assays, where we used a set of 7 cannabinoid ligands (both
- 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
- 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
- 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
- Scientific Isolation: The Real Reason Early Biotechs Lose Traction
it looks like in real life: Meetings end with explanations, not decisions BD calls “went great,” but nothing
- 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
- 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





