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Learn binding, bias, kinetics, and core models—fundamentals that fuel confidence and fluency Move beyond

The reagents are compatible with HTRF readers  and validated in GLP1R  and Mu opioid receptor (MOR)  models

of the most recent findings in human studies and contextualize them considering previous preclinical models

Xenograft mouse model was generated to investigate the in vivo efficacy of fentanyl.

Are You Using Models That Slow You Down?  

high-resolution techniques to investigate peptidergic transmission and expression throughout the brain in model

most significant groups of G-protein coupled receptor (GPCR) drug targets and also act as prototypical models

residues that influence efficacy and potency, pharmaceutical researchers can create drugs that precisely modulate The study distinguishes between driver residues , which directly influence signal transduction, and modulator Alternatively, allosteric modulators , which bind to sites outside the traditional ligand-binding pocket Allosteric modulators offer a promising approach for developing drugs that enhance or inhibit receptor within the ligand-binding pocket, resulting in a significant opportunity for developing allosteric modulators

The choice of model systems, such as yeast, bacteria, or mammalian cells, can heavily influence the method's Additionally, combining DMS with computational modelling and machine learning algorithms promises to

Our model not only shows the function of dimeric β2-AR but also provides a molecular insight into the

subcellular localization and activity in a polarized epithelium using the Drosophila wing imaginal disc as a model

tuberculosis adenylyl cyclase (AC) Rv1625c/Cya is an evolutionary ancestor of the mammalian membrane ACs and a model

Our model not only shows the function of dimeric β2-AR but also provides a molecular insight into the

In a LPS-induced lung inflammation model in mice, ACT-660602 led to significantly reduced recruitment

CXCR1/2 inhibitors show beneficial effects in various animal models of CVD.

CXCR1/2 inhibitors show beneficial effects in various animal models of CVD.

Our data support a model wherein Smog regulates distinct myosin pools and actin cytoskeleton in a ligand-dependent

In a mouse model of contact hypersensitivity, β-arrestin-biased CXCR3-mediated inflammation is dependent

Our data support a model wherein Smog regulates distinct myosin pools and actin cytoskeleton in a ligand-dependent

Tissue responses defied the model. effects often originate in precise brain regions, not just the pancreas This tool helped clarify: Which neurons

We discuss the importance of understanding the translatability of cell and animal models to have more

The absence of VLGR1 in tissues and cells derived from VLGR1-deficient mouse models resulted in alterations

These data lead us to a model where Kel1 promotes completion of cytokinesis before pheromone-induced

These data support a model where Gq and Gβγ-dependent signaling cooperatively regulate PLC activation

Using shRNA knockdown and CRISPR/Cas9 knockout cell lines, as well as mouse models, we confirmed the

the discovery process, including its pioneering organellar electrophysiology platform, iPSC-derived models

Recently, Suchismita Roy et al. have explored how growth factors can modulate canonical G protein signaling primary research question addressed in this study was: How do growth factors, specifically through RTKs, modulate The ability of growth factors to modulate G protein signaling through specific phosphorylation events inform the development of therapeutic strategies aimed at targeting specific phosphorylation events to modulate

Moreover, the main investigations into animal models and ongoing clinical trials using these unimolecular

In this study, we established an experimental Sjögren's syndrome (ESS) mouse model to elucidate the molecular increased saliva flow, alleviated salivary gland indices, and improved tissue integrity in the ESS model

An alternative and promising approach is allosteric modulation. Over the past decade, there has been a notable growth in the discovery of allosteric modulators for GPCRs which possess the capability to modulate and fine-tune the affinity and/or efficacy of orthosteric ligands Allosteric modulators that do not exhibit agonistic properties remain inactive in the absence of endogenous In this context, allosteric modulators exhibiting constrained positive or negative cooperativity are