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- 📰 GPCR Weekly News, February 13 to 19, 2023
Mandibulofacial dysostosis with alopecia results from ETAR gain-of-function mutations via allosteric
- Extracellular signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery
ERK activation pathways can be categorised into two main sub-pathways based on their subcellular localisation
- Unlocking the Therapeutic Potential of Previously Undruggable GPCRs
remaining non-sensory receptors, with functions more readily linked to pathology, are currently the main cell surface, or because they have an enhanced capacity to elicit receptor internalization, thereby gaining 17706–17711. https://doi.org/10.1073/pnas.0805098105 · Development and use of new technology to gain
- Beyond Clearance: The Strategic Power of Irreversible Drug Binding
In this lesson, you'll gain: ✅ Clarity on what “irreversible” really means in kinetic and pharmacologic
- From DNA day to GPCR genomics
The G-protein-coupled receptors in the human genome form five main families.
- Assay Sensitivity: The Hidden Lever Driving GPCR Drug Discovery
In this course, you’ll gain: ✅ How assay volume control alters receptor sensitivity and what that
- 📰 GPCR Weekly News, September 25 to October 1, 2023
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- Biased Agonism at the GLP-1 Receptor: A Pathway to Improved Therapeutic Outcomes
This concept is gaining significant attention in drug discovery, especially in the context of G protein-coupled
- From Snapshots to Predictions: Why Mechanism of Action Matters
In This Session, You’ll Gain: ✅ How to turn descriptive snapshots into predictive insights ✅ Tools to What looked like four conflicting behaviors turned out to be one coherent mechanism , hidden in plain
- How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology
animals — a milestone that demonstrated just how powerful well-engineered chemical tools can be when paired JB gained a grounded understanding of tissue heterogeneity, signal variability, and the biology that
- Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls
In this session, you’ll gain: Why saturation and displacement assays fail when protein stoichiometry
- GPCR Pharmacology Insights That Prevent Real Drug Discovery Failures
In this session, you’ll gain: How system sensitivity transforms potency, efficacy, and agonist classification
- Chemokine receptor-targeted drug discovery: progress and challenges
inappropriate target selection and insufficient dosing of chemokine receptor antagonists in vivo might be the main
- From Failed Experiments to Predictive GPCR Models
His introduction came through a practical suggestion: explore a new protein family that was gaining traction
- The Real Cost of Strategic Overload in Biotech
What did you decide not to pursue to strengthen the main thesis?
- The Moment Biotech Founders Realize the Money Is Gone
and partnerships are delayed, not by strategy, but by fear of cash burn 4️⃣ Fundraising becomes the main
- Targeting Intracellular Allosteric Sites in GPCRs
Allosteric modulation is gaining prominence in GPCR therapeutics, with the discovery of an intracellular
- High-Content Screening for GPCR Programs: Overcoming Assay Limitations with Fluorescent Ligands
Non-Radioactive Workflow By removing isotopes, researchers gain safer, more scalable, and more environmentally
- Odorant receptors – a bit of smell for drug discovery
In the cardiovascular system, ORs have the potential to operate as the main carriers of endogenously
- Artificial intelligence – faster, smarter, cheaper GPCR drug discovery
The future According to the authors, the future of AI relies in 6 main areas: 1.
