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Results found for "Nyla Naim"
- Reversible Photocontrol of Dopaminergic Transmission in Wild-Type Animals
Azodopa is the first photoswitchable dopamine agonist with demonstrated efficacy in wild-type animals
- G protein-coupled receptors that influence lifespan of human and animal models
we present the analysis of a series of GPCRs whose activity has been shown to affect the lifespan of animal
- Finding needles in haystacks: Omass unveils pipeline aimed at tough-to-drug targets
structure-based technology has passed a key test, in enabling the discovery of orally available small molecules aimed
- GPCR Pharmacology Insights That Prevent Real Drug Discovery Failures
Orthosteric dose increases drive continuously stronger responses; NAMs and PAMs have structural ceilings For complex GPCR systems, this boundary is a strategic advantage: NAMs can only shift an agonist curve NAMs, PAMs, and Subtle Mechanistic Traps Modulators are frequently labeled correctly but characterized Kenakin stressed that low-alpha NAMs can resemble competitive antagonists unless deeper kinetic or concentration-range
- Building Backwards: Why Top-Down Models Could Revolutionize Pain Research
170 Thinking Differently Pain research has long followed a familiar route: from molecule, to cell, to animal In his work, Serafini emphasizes a phenotype-driven, patient-relevant perspective , where animal models
- How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology
probes precise enough to visualize the receptor across islets, tissue slices, and ultimately living animals Two-photon microscopy experiments showed GLP-1R signaling in intact animals — a milestone that demonstrated performing increasingly complex imaging experiments that capture receptor dynamics in intact tissue and live animals
- Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
CXCR1/2 inhibitors show beneficial effects in various animal models of CVD.
- Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
CXCR1/2 inhibitors show beneficial effects in various animal models of CVD.
- Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology, behavior...
We discuss the importance of understanding the translatability of cell and animal models to have more
- Keratinocyte-derived defensins activate neutrophil-specific receptors Mrgpra2a/b to prevent skin...
Def and Mrgpra2 mutant animals both exhibited skin dysbiosis, with reduced microbial diversity and expansion
- Novel Therapies for Cardiometabolic Disease: Recent Findings in Studies with Hormone...
Moreover, the main investigations into animal models and ongoing clinical trials using these unimolecular
- GRK2 in cardiovascular disease and its potential as a therapeutic target
and summarizes the ongoing and future research for targeting this critical kinase across cellular, animal
- Induced Human Regulatory T Cells Express the Glucagon-like Peptide-1 Receptor
Recent studies in experimental animals have shown that certain subsets of T cells express functional
- GPCR voltage dependence controls neuronal plasticity and behavior
This voltage dependent potentiation is abolished in mutant animals expressing a voltage independent receptor
- Differences across sexes on head-twitch behavior and 5-HT2A receptor signaling in C57BL/6J mice
compared to male C57BL/6J mice, a sex-specific exacerbated behavior that was not observed in 129S6/SvEv animals
- A new Kunitz-type snake toxin family associated with an original mode of interaction with the...
original mode of interaction with the vasopressin 2 receptor "Abstract Background and purpose: Venomous animals We aimed to exploit other mamba venoms to enlarge the V2R-Kunitz peptide family and gain insight into
- Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water ...
identification of GPCR genes can provide insight into the adaptive strategy and evolutionary tendency in an animal
- Target Residence Time: The Hidden Driver of In Vivo Efficacy
Residence time provides a second dimension of drug evaluation , one that explains results in animal models
- Structural dynamics of Smoothened (SMO) in ciliary membrane and its interaction with membrane lipids
which is involved in embryonic development and is implicated in various types of cancer throughout the animal
- How System-Level GPCR Thinking Prevents Discovery Failures
is where system-level GPCR thinking becomes a competitive advantage—long before a molecule reaches animals Avoid misleading mechanistic labels → NAMs, PAMs, and biased agonists behave in system-dependent ways
- The Five Traps of Ignoring Kinetics
in calcium assays to rapidly rank offset rates, and predict in vivo coverage before you ever dose an animal
- 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
- Accelerating GPCR Drug Discovery: What 40 Years of Pharmacology Reveal
Early cross-screening can flag biased phenotypes long before animal studies.
- The mouse cytomegalovirus G protein-coupled receptor homolog, M33, coordinates key features of ...
Animal models of CMV provide insights into their role in viral fitness.
- Extracellular signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery
“The desire to take medicine is perhaps the greatest feature which distinguishes man from animals.”
- Assay Sensitivity: The Hidden Lever Driving GPCR Drug Discovery
Every mischaracterized compound that enters animal studies or early trials is a tax on time and resources
- 📰 Breaking Down the Latest GPCR Discoveries: a Weekly Update (Nov 27-Dec 3, 2023)
apoptosis Methods & Updates in GPCR Research Modulating signalling lifetime to optimise a prototypical animal
- GPCR Buzz of the Week | Sep 23 - 29, 2024
drugs for pain Reviews, GPCRs, and more The role of G protein-coupled receptors and their ligands in animal
- 📰 GPCR Weekly News
High-performance optical control of GPCR signaling by bistable animal opsins MosOpn3 and LamPP in a molecular
- Unlocking the Therapeutic Potential of Previously Undruggable GPCRs
Orion’s receptor antagonist analogs have demonstrated powerful efficacies across a range of animal models











