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Picture this: two compounds bind to the same receptor. One sparks a firestorm of cellular activity. Terry walks you through real-world experiments, decades of receptor pharmacology wisdom, and the cutting-edge

Celtarys Research expands its assay tools with CELT-419 for D3 receptor studies, and Dr. Terry Kenakin brings translational clarity to complex receptor concepts.   Platforms   Celtarys Research presents CELT-419, a nanomolar-affinity fluorescent ligand optimized for D3 receptor Highlights     Phosphorylation selectively regulates β-arrestin recruitment  across glucagon family receptors

University of Michigan, walks us through how positive allosteric modulators (PAMs) targeting the mu-opioid receptor That’s huge.” – Ben Clements By combining chronic pain models with receptor-level pharmacology, Ben Allosteric modulation is already proven in ion channels (think benzodiazepines and barbiturates) but University today. _______________ Keyword Cloud: GPCR research community, GPCR drug discovery, mu-opioid receptor

correlation network analysis (WGCNA) were performed using R software, and functional enrichment analysis and protein–protein

Fast-forward a few thousand years, and we’re talking beta receptors, receptor theory, and AI-generated

will focus on the application of artificial intelligence (AI), machine learning, and the design of protein of Oxford, where she is currently Professor of Structural Bioinformatics and leads the University’s Protein

For GPCR-focused programs, the ability to visualize receptor localization, internalization kinetics, The resulting multiparametric datasets are well-suited for GPCR research, where receptor trafficking, For GPCR assay developers, HCS supports:  Quantitative visualization of receptor internalization and Their ability to visualize ligand–receptor interactions directly in living cells produces data that are advantages include: Physiological Relevance Fluorescent ligand binding occurs in intact cells, preserving receptor

47th Symposium on Hormones & Cell Regulation; new approach to GPCR internalization analysis; “Soluble Proteins Target protected agonism:  Internalized MT2 signaling escapes AGRP antagonism—unlike α-MSH. Dual-label specificity blocks promiscuous ligand confusion Lanthanide donors + d2 acceptors = high SNR

It will bridge foundational receptor theory with today’s most pressing pharmacological questions, from Kenakin   Four decades of receptor theory now fit in one expert-guided hub.

He’s focused on RGS proteins , pain comorbidities  like addiction and depression, and pushing for more

ATP and sugar monophosphates and the identification of a novel allosteric site on the vasopressin V2 receptor Discover how factors like restricted tissue diffusion and receptor density can dramatically alter drug Learn how fentanyl slows inhalation via opioid receptors, while xylazine prolongs exhalation through alpha-2 adrenergic receptors, creating a synergistic effect that drives overdose deaths.

In this session, you’ll gain: ✅ A clear breakdown of how intracellular vs. extracellular receptor access In this protected environment, pharmacokinetics can decouple from plasma clearance. GPCRs Aren’t Just Surface Receptors Anymore From β2-adrenoreceptors to CCRs and dopamine receptors, multiple

Depending on which ligand activates a receptor, it can engage different intracellular transducers. 'biased signalling' paradigm requires that we now characterize physiological signalling not just by receptors but by ligand-receptor pairs. The guidelines will aid consistency and clarity, as the basic receptor research and drug discovery communities

Revered for its convenience, the FLIPR assay provides rapid insights into receptor activity.

trisphosphate, which are downstream signal transducers for the expression of fetal genes, increased protein

Abs against the angiotensin II receptor subtype 1 (AT1R) and the endothelin receptor type A (ETAR) are Promising nuclear receptors as key regulators of transcriptional programmes will be introduced as well

By targeting the receptors synaptically or non-synaptically, neurotransmitters activate multiple signaling Significantly, many ligands acting on neurotransmitter receptors have shown great potential for inhibiting

Reading those first papers on GPCR signaling organization absolutely fascinated me — the idea that receptors to integrated signaling landscapes, accelerating drug discovery timelines and expanding targetable receptor

Her early work didn’t involve groundbreaking receptor models or million-dollar grants. within the Drug Discovery Biology theme at Monash Institute of Pharmaceutical Sciences, exploring how receptors

Dopamine receptors are involved in the modulation of fundamental physiological functions, and dysregulation We demonstrate that azodopa activates D1-like receptors in vitro in a light-dependent manner.

yesterday for contributions to the field of mass spectrometry and establishing it as method to analyse proteins

upstream of the agonistic peptide sequence, an event necessary for NTF displacement and subsequent receptor phenocopies the pulmonary phenotype of GPR116 knock-out mice, demonstrating that tethered agonist-mediated receptor

partner GlaxoSmithKline PLC posted results Dec. 7 demonstrating activity against the omicron spike protein

tagging to scalable multiplex assays, this conversation dives deep into the tools now transforming receptor

flipped that logic: Shared infrastructure, not duplicated equipment Centralized core facilities for receptor That gave them capabilities others couldn’t match — from receptor biosensor platforms to live-cell imaging

Glutamate exerts its effect through ionotropic and metabotropic glutamate receptors (mGluRs). mGluR2 drug targets for the treatment of many neurological conditions and several compounds targeting these receptors

behavior of salivary adenoid cystic carcinoma via the PI3K/AKT signaling pathway "Background CC chemokine receptor 9 (CCR9), an organ-specific chemokine receptor, interacts with its exclusive ligand CCL25 to promote

. ✅ Future-proof your career: Conquer complex laws and understand where receptor theory is going next

Current progress in our knowledge of the itch processing, the numerous mediators and receptors involved Currently, inhibitors of IL-31, IL-4/13, NK1 receptors, opioids and cannabinoids, JAK, PDE4 or TRP are

We show that locally restricted suppression of postsynaptic cAMP levels or of cAMP-dependent protein-kinase