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Results found for "Luke Pattison"
- A Setmelanotide-like Effect at MC4R Is Achieved by MC4R Dimer Separation
In summary, our study shows that inhibiting homodimerization has a setmelanotide-like effect on Gq/11
- Lysosomal GPCR-like protein LYCHOS signals cholesterol sufficiency to mTORC1
Cholesterol bound to the amino-terminal permease-like region of LYCHOS, and mutating this site impaired
- Increased Anxiety-like Behaviors in Adgra1-/- Male But Not Female Mice are Attributable to...
October 2022 Increased Anxiety-like Behaviors in Adgra1-/- Male But Not Female Mice are Attributable
- Mechanism of enhanced sensitivity of mutated β-adrenergic-like octopamine receptor to amitraz in...
October 2022 Mechanism of enhanced sensitivity of mutated β-adrenergic-like octopamine receptor to amitraz Previous assays verified that a typical G protein-coupled receptor, β-adrenergic-like octopamine receptor
- Induced Human Regulatory T Cells Express the Glucagon-like Peptide-1 Receptor
September 2022 "The glucagon-like peptide-1 receptor (GLP-1R) plays a key role in metabolism and is an
- A2B Adenosine Receptor Enhances Chemoresistance of Glioblastoma Stem-Like Cells under Hypoxia: New..
September 2022 A2B Adenosine Receptor Enhances Chemoresistance of Glioblastoma Stem-Like Cells under and the presence of a cell subpopulation that persists under hypoxic niches, called glioblastoma stem-like
- TLR4 biased small molecule modulators
Toll-like receptor 4 (TLR4) is one such non-GPCR receptor, which involves MyD88-dependent and TRIF-dependent
- Divergent roles for the gut intraepithelial lymphocyte GLP-1R in control of metabolism, microbiota..
cell-induced inflammation "Gut intraepithelial lymphocytes (IELs) are thought to calibrate glucagon-like
- 🎄 Have Yourself a Merry Little GPCRmas! ❄ Dec 9 - 15, 2024
Activation of the proton-sensing GPCR, GPR65 on fibroblast-like synoviocytes contributes to inflammatory joint pain Luke A Pattison , Rebecca H Rickman , Graham Ladds , Ewan St John Smith , et al. Biologist GPCR Activation and Signaling Activation of the proton-sensing GPCR, GPR65 on fibroblast-like
- 📰 GPCR Weekly News, October 2 to 8, 2023
silico identification of a biarylamine acting as agonist at human β3 adrenoceptors and exerting BRL37344-like malformations by endothelial activating GPR4 signals GPCRs in Neuroscience Involvement of a silkworm D2-like Development DKK 25 million to development of databases supporting medical research ‘Define your own success’: Duke
- The Quiet Power of RGS Proteins: Rethinking Pain Pathways through GPCR Biology
Serafini described his connection to GPCRs as tangential but inevitable: "I feel like I never was particularly intriguing because it was expressed robustly both in the peripheral nervous system and in central circuits like highlighted that in modern pain drug development, the field has remained too focused on ion channels like downstream cascade is probably a little bit weaker than if you were hitting a GPCR... and honestly, like
- From Snapshots to Predictions: Why Mechanism of Action Matters
Instead of saying, “This looks like partial agonism” , you can ask: What happens if concentration increases Without the right model, it’s like staring at identical twins—you can’t tell them apart until you see Without a framework, this looks like an assay error. What looked like four conflicting behaviors turned out to be one coherent mechanism , hidden in plain a shift,” “seems like baseline activation”—you’re leaving risk on the table.
- Why “Displacement” Misleads You: Allosteric Binding Demystified
If you’re applying orthosteric logic to modulator-driven systems, you’re likely misreading your assays—and You’ll learn how to recognize these shifts using vivid analogies (like Bruce Wayne vs. Kenakin shows how even small cooperativity values (like α = 0.1) cap the shift in signal . The takeaway: what looks like pharmacology failure may be a systems problem . If you’re still using orthosteric assumptions to interpret allosteric binding data, you're likely missing
- What If Your Data is Lying to You? The Calcium Assay Dilemma
Through real-world examples (like 5-HT2A and CCR5 agonists), Terry shows how slow-onset agonists can Because when true pharmacological profiling is essential—like detecting partial or inverse agonism—calcium
- Building Backwards: Why Top-Down Models Could Revolutionize Pain Research
This approach reflects his focus on developing models that behave like patients before molecular exploration hypothesis, Serafini’s team noticed that hamsters infected with SARS-CoV-2 exhibited persistent pain-like He also integrates concepts like sex differences , epigenetic inheritance , and neuroimmune crosstalk
- Biased Agonism at the GLP-1 Receptor: A Pathway to Improved Therapeutic Outcomes
significant attention in drug discovery, especially in the context of G protein-coupled receptors (GPCRs) like the glucagon-like peptide-1 receptor (GLP-1R). As our understanding of the molecular basis of biased agonism continues to grow, it is likely to play Drucker, D.J., Mechanisms of Action and Therapeutic Application of Glucagon-like Peptide-1. AZIETAKU, J.T., Profiling Glucagon-Like Peptide -1 Receptor Transducer Coupling, Signalling and Biased
- Purpose-Driven Opioid Research: Catherine Demery’s Academic Path
Like many young scientists, she explored different paths and gained industry experience before realizing The work no longer felt like an assignment—it felt like a calling. “I really like academia. about having the freedom to pursue questions that matter—questions tied to urgent public health crises like
- Conjugation Strategies for Probe Development
In this case, we would like to focus on the synthesis of fluorescent probes. has several advantages: it is usually very robust, good yields, reagents are found in most chem labs (like Not only do they work in aqueous medium, but also in aprotic solvents like DMF, where you will need to It also poses some disadvantages – just like acid-amine amide coupling, some byproducts are obtained
- How Understanding Intracellular Drug Access Can Transform Your GPCR Drug Discovery Program
Breakthroughs this week: Glucagon-like Peptide-1 Receptor (GLP-1R) Signaling; Proximity-Dependent Proteomics He shares his journey into computational chemistry and offers a compelling look at how tools like AlphaFold Harness the power of AI: Discover how breakthroughs like AlphaFold are making previously "undruggable " targets, like olfactory receptors, accessible for computational analysis. Connect with experts: Join a community of like-minded field-experts dedicated to improving our collective
- Lab Leadership Without Ego: How Sokhom Pin Built the Happiest Team at Alkermes
In a field like GPCR research (where data complexity and failure rates are high), scientific rigor thrives Alkermes didn’t just improve drug screening outcomes, it redefined what great leadership in biotech looks like
- Class B1 GPCR Dimerization: Unveiling Its Role in Receptor Function and Signaling
While GPCRs can exist as monomers, some types, like class C GPCRs, are obligate dimers, either as homodimers For example, dimerization has been shown to affect signaling pathways in class A dopamine receptors like Research using techniques like bioluminescence resonance energy transfer (BRET) and fluorescence resonance Graaf, C., et al., Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March Schelshorn, D., et al., Lateral allosterism in the glucagon receptor family: glucagon-like peptide 1
- How a Failed Experiment Created a Powerful GPCR Imaging Tool
This was the moment when photopharmacology felt like the future. The literature was buzzing. For metabolic GPCRs (like GLP-1 and GIP receptors): Drug efficacy depends on which cells express the And importantly, they liked working together.
- From Lab Logic to Leadership: How Scientific Thinking Holds Back Biotech Operations
. 👉 Most founders don’t even realize they’re still running their company like an academic research group Founders who keep operating like researchers often create internal confusion. Leadership isn’t in your lab notebook; it’s in how you decide How to Know If You're Still Leading Like And if your thinking is still shaped by academic norms, your startup will keep running like a lab, not
- How GPCR Spatial Signaling Sparked a Scientific Journey
For Early-Career Scientists: Your pivotal moment might not feel like fireworks. For innovators and biotech strategists, stories like Michelle’s reveal how scientific leadership emerges For GPCR research, leaders like Michelle are showing what happens when we follow the signal all the way
- Misread the Curve, Misjudge the Drug: Rethinking Antagonism in GPCR Pharmacology
If the maximal response drops, non-competitive seems like the obvious answer. Terry also explores the experimental constraints —like timing and equilibrium—that determine whether He challenges the idea that curve shape alone is diagnostic, pointing out how features like receptor
- GPCR Allosteric Modulation: Why Allostery is the Engine of Drug Discovery
These sites don’t behave like traditional active sites. Why “Affinity Alone” Isn’t Enough—Again Just like binding kinetics require us to go beyond static Kd Terry’s Pharmacology Corner delivers trusted, razor-sharp insight to help drug discovery professionals like
- Assay Sensitivity: The Hidden Lever Driving GPCR Drug Discovery
Assay sensitivity is like adjusting the brightness on a microscope—set it right, and hidden details jump Think of it this way: most receptors behave like switches—they stay off until flipped. But some leak current, like a switch glowing faintly in the dark. Model patient-like pathophysiological states (e.g., reduced receptor expression in heart failure).
- Is Your Agonist Really “Working”—Or Are You Just Seeing What Your System Allows?
. 👉 Dive into Terry’s Vault and see agonism like never before Unlock "Agonism & Sensitivity" now
- From Farm Fields to GPCR Discovery, GLP-1 and GIP
Those courses didn’t feel like career-defining moments at the time — just requirements to pass. Hodson made what seemed like a purely tactical decision: choose a research elective to focus on exams They start with people you actually like working with .
- FDA Approval Is a Strategy Obstacle, Not a Paperwork Problem
solid preclinical package, promising safety data, and a consistent in vivo proof-of-concept, it feels like What the FDA Is Actually Optimizing For 👉 Biotech teams often treat the FDA like an evaluator. In reality, the FDA acts more like a systems-level risk assessor . indication selection to study design, should be filtered through the question: “What would this look like



















