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Results found for "Howard Hughes"
- Dr. GPCR and Celtarys Research Join Forces to Expand Access to Innovative GPCR Tools
Celtarys Research develops high-quality, fluorescently labeled ligands and innovative chemical biology These tools enable high-resolution binding studies, kinetic analysis, and live-cell imaging, empowering “We’re thrilled to partner with Celtarys and introduce their high-performance fluorescent ligands to
- Why Opposing Processes Matter for Your Next GPCR Drug
If your job is to move molecules confidently toward the clinic, this is a blueprint for building a more This insight has huge implications for how you select and rank agonists in discovery campaigns.
- Applications of Fluorescent Probes in Confocal Imaging of GPCRs: From Live to Fixed Cells
To make the most out of this imaging technique, fluorescent probes must have high specificity, minimal How Fluorescent Probes Enable High-Resolution Confocal Imaging of GPCRs To study the dynamics of GPCRs PerkinElmer High Content Analysis System Operetta CLS used by a Celtarys Research coworker. A High Content Screening focused microscope that has a confocal-like mode as well.
- PH-Binding Motif in PAR4 Oncogene: From Molecular Mechanism to Drug Design
Pc(4-4), a lead backbone cyclic peptide, was selected out of a mini-library, directed toward PAR2&4 PH-binding We propose that Pc(4-4) may serve as a powerful drug not only toward PAR-expressing tumors but also for
- Optimizing HTRF Assays with Fluorescent Ligands: Time-Resolved Fluorescence in GPCR Research
Overcoming Common Challenges Balancing sensitivity and scalability is one of the hardest challenges in high-throughput one is limited by radioactivity-related safety and environmental concerns, while the other one has high utilized our fluorescent ligand, CELT-335 , designed for hCB 1 /CB 2 cannabinoid receptors, demonstrating high Celtarys enhances the power of HTRF and other FRET-based technologies by providing high-performance in GPCR biology with advanced fluorescence chemistry, Celtarys custom-developed ligands offer both high
- From Technician to Trailblazer: How Sokhom Pin Designed His Own PhD Program While Working in Industry
Sokhom met weekly with advisors and monthly for presentations All research was publication-quality, high-impact that were scientifically sound and directly publishable, a skill honed from years of hands-on work in high-throughput
- Overview of adhesion GPCRs self-activation
Through cell-based assays and Cryo-EM of high quality, it was possible to know that ADGRL3 can activate where Gi had the fewest hydrophobic and polar interactions with the receptor and the αH5 tilt of G12 towards G-protein coupling, since the change of amino acids in positions close to this position favored signaling toward
- 📰 GPCR Weekly News, August 28 to September 3, 2023
Reveals Insights into the Energy Landscape of the Molecule Focused classifications and refinements in high-resolution Industry News Septerna Bolsters Leadership Team as the Company Advances its Multi-Product Pipeline Toward
- Therapeutic validation of an orphan G protein‐coupled receptor
there is still a lot to be done in respect to tool compounds to study the function of this receptor towards allosteric modulator of GPR84, a metabolite produced in vivo from indole‐3‐carbinol, which is present at high
- 📰 GPCR Weekly News, July 31 to August 6, 2023
emerging methods for probing neuropeptide transmission Nanowire Biosensors with Olfactory Proteins: Towards a genuine electronic nose with single molecule sensitivity and high selectivity Reviews, GPCRs, and
- Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls
and displacement assays fail when protein stoichiometry shifts How two-stage GPCR binding creates “high A displacer appears weaker at high tracer occupancy because more ligand must be displaced. That second step stabilizes a higher-affinity configuration, explaining classical “high” and “low” affinity The high-affinity state is undersupported, creating biphasic curves. High receptor levels also deplete free tracer when tracer concentrations are low, breaking the assumption
- GPCR Happy Hour – Boston, Sept 2025
include AI-driven target identification, target validation, assay development, compound management, and high-throughput Screening campaigns can be performed using Axxam’s high-quality compound collections—both synthetic and including its pioneering organellar electrophysiology platform, iPSC-derived models, optogenetics, and high-content
- How Collaboration Drives GPCR Discoveries
The shift toward team science isn’t cultural. It’s technical. This is where GPCR science is heading: toward deeper integration, shared tools, and partnerships that
- VAMP2: a crucial player in the delivery of MOR to the synapse
the SNARE complex, including vesicle-associated membrane protein 2 (VAMP2), regulate this last step toward Through developing a high-resolution method, Hao Chen et al. directly visualized the fusion of vesicles
- InterAx Biotech AG and Boehringer Ingelheim take collaborate to unlock orphan targets leveraging ...
February 2022 "InterAx Biotech AG and Boehringer Ingelheim take first steps towards collaborating to
- Molecular targets of psychedelic-induced plasticity
of a psychedelic drug becoming again an approved treatment, much of these efforts have been oriented toward
- Do You Believe AI Could Accelerate Drug Discovery?
They found that AF2 models achieved accurate side-chain predictions and successfully docked high-affinity receptor, AF2 models showed some variations at key residues, and docking 1.6 billion molecules resulted in high 5-HT2A, 5-HT2B, and 5-HT2C receptors, with several compounds demonstrating subtype selectivity and high To fully harness these benefits, it is essential to keep updating and refining the databases with high-quality
- Signals in Motion: Pain, Metabolism & Terry’s Corner
publication highlights: CXCR4 takes on a nuclear role in red blood cell maturation CXCL13/CXCR5 emerges as a high-potential Radioligands – Assay Smarter Celtarys explores how fluorescent ligands enable safer, high-throughput
- N-terminal alterations turn the gut hormone GLP-2 into an antagonist with gradual loss of GLP-2 ...
alterations turn the gut hormone GLP-2 into an antagonist with gradual loss of GLP-2 receptor selectivity towards
- The Hidden Driver of GPCR Drug Success: Why Target Residence Time Matters More Than You Think
Career opportunities: Explore a selection of high-level job openings in high-throughput screening, research Competitive Edge: Identify high-value compounds that might be missed by traditional screening methods Amplify your work with high-impact visibility.
- Unlock the Hidden Complexity Behind GPCRs—From Terry Kenakin’s Vault
It’s 40 years of hard-won insight distilled into accessible, high-impact content designed for learners
- Understanding Orthosteric Binding: The Key to Drug Action
A high affinity means the drug will bind more easily and effectively. Often, a low EC50 indicates high potency, but this isn't always the case due to various biological factors
- Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
Much focus is currently being directed towards CXCR1/2 inhibitors, as these receptors primarily induce
- Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
Much focus is currently being directed towards CXCR1/2 inhibitors, as these receptors primarily induce
- From Failed Experiments to Predictive GPCR Models
While others refined lab techniques, he found himself gravitating toward structural models in his spare This scarcity made the field both exciting and high-risk.
- Dr. GPCR Spotlights Revvity’s pHSense™ Internalization Tools
persistent barriers in internalization studies : Complex imaging workflows Limited scalability for high-throughput readouts – phospho-ERK, AKT, CREB, MEK and other phoshoproteins These reagents are optimized for high-throughput
- Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology, behavior...
is intriguing that many results emerged from behavioral and physiological studies implying that bias toward
- Artificial intelligence – faster, smarter, cheaper GPCR drug discovery
High-throughput approaches used in drug discovery create large datasets regarding ligand synthesis and when searching for novel receptor ligands, as “ligand-based approaches often bias molecule generation towards Towards a comprehensive understanding of GPCRs, ligands, diseases, and their associations: open-access
- Fluorescence based HTS compatible ligand binding assays for dopamine D3 receptors in baculovirus preparations and live cells
Budded baculoviruses (BBV) have a high receptor concentration as well as being homogenous in size, which D3 receptor, and there is a large difference between total and non-specific binding resulting in a high CELT-419 has the properties required for measuring affinities of unlabeled ligands: good affinity, high The assay shows a high signal level with DELTAFA+-SD between total and non-specific points of 0.12+-0.02 Structure-Based Design of High-Affinity Fluorescent Probes for the Neuropeptide Y Y1 Receptor. J.
- Decoding GPCR Function: The Role of Mutagenesis in Rational Drug Discovery
For example, random mutagenesis, combined with novel specificity high-throughput selection, has been Integrating mutagenesis data with computational models also presents challenges, requiring high-quality To overcome these challenges, future directions include developing high-throughput techniques, better Future advancements, including high-throughput techniques and bioinformatics integration, will further

















