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- Target Residence Time: The Hidden Driver of In Vivo Efficacy
In This Session, You’ll Gain: ✅ Modeling tools to understand how restricted diffusion in tissues like
- How GPCR Spatial Signaling Sparked a Scientific Journey
Pay attention to that. What began as a quiet obsession soon demanded a bigger stage. control localised signaling, how disease hijacks these systems, and how to target them for therapeutic gain
- Why “Displacement” Misleads You: Allosteric Binding Demystified
In This Session, You’ll Gain: ✅ A clear explanation of why allosteric modulators don’t displace ligands—they
- Differential binding of Δ9-tetrahydrocannabinol derivatives to type 1 cannabinoid receptors (CB1)
Introduction Cannabinoid receptors are GPCRs, and two main types exist, CB1R and CB2R.
- Why Intracellular Drugs May Hold the Key to GPCR Therapeutics
In this session, you’ll gain: ✅ A clear breakdown of how intracellular vs. extracellular receptor access
- Role of G Protein-Coupled Receptors in Hepatic Stellate Cells and Approaches to Anti-Fibrotic ...
Gaining control over disease-related events in non-alcoholic steatohepatitis (NASH), an advanced form
- Early Safety Assays: Identifying Showstoppers in GPCR Drug Discovery Pipelines Early
In this session, you’ll gain: Clarity on high-impact early safety assays and their compelling rationale
- Characterization of a new WHIM syndrome mutant reveals mechanistic differences in regulation of ...
While several gain-of-function mutations that lead to C-terminal truncations, frame shifts and point
- The Hidden Operating Cadence That’s Actually Driving Your Biotech
Many early-stage biotechs show the same pattern: strong scientific progress paired with an operating discipline, the organization typically shifts from “busy but slightly lost” to “focused, aligned, and gaining
- How System-Level GPCR Thinking Prevents Discovery Failures
What You’ll Gain Spot false confidence early → Sensitivity differences can turn full agonists into partials
- Structural dynamics of Smoothened (SMO) in ciliary membrane and its interaction with membrane lipids
the interactions of SMO with cholesterol and other lipid molecules in the ciliary membrane, and to gain
- How GPCR Collaboration Built an Innovation Engine
Monash team built rotational PhD cohorts — students cycled through multiple groups in their first year, gaining
- How to Use Statistical Methods to Strengthen Every GPCR Drug Discovery Decision
Gain career inspiration from Ajay’s bold questions and pivots.
- Dimerization of GPCRs: Novel insight into the role of FLNA and SSAs regulating SST2 and SST5...
receptors (SSTs) are class A GPCRs abundantly expressed in pituitary tumors where they represent the main
- Purpose-Driven Opioid Research: Catherine Demery’s Academic Path
Like many young scientists, she explored different paths and gained industry experience before realizing
- Better GPCR Drug Discovery Decisions Start With Structured Learning
What you gain: Detect scaffold liabilities early—hERG inhibition, mutagenicity, and mechanistic red flags
- Why Mastering Pharmacokinetics Fundamentals Still Defines Discovery Success Today
In This Session, You’ll Gain Clarity on how ADME governs translational success A deeper understanding
- Targeted Drug Design through GPCR Mutagenesis: Insights from β2AR
Deep mutational scanning, for instance, is gaining popularity as a strategy due to its ability to comprehensively
- Curve Shifts Don’t Lie, But Your Eyes Might
In This Session, You’ll Gain: ✅ The ability to calculate how many replicates you really need for 95% By comparing two means (paired or unpaired) you’ll learn whether the divergence is genuine or whether
- Your GPCR Program Decisions Depend on Good Data Interpretation
GPCR Premium Members this week gain curated, early access to: Industry insights : GPCRs and mRNA in drug At Alkermes, Sokhom Pin built an in vitro pharmacology group from scratch—not just a lab, but a culture
- Decoding Schild Analysis: The Pharmacologist’s Lens on Competitive Antagonism
In this session, you’ll gain: A clear conceptual map of Schild analysis and its origins.
- Accelerating GPCR Drug Discovery: What 40 Years of Pharmacology Reveal
In this session, you’ll gain: ✅ Proven strategies to balance in vitro vs. in vivo testing early — when
- Orthosteric vs. Allosteric Interactions: The Silent Decider of Safety and Success
In this session, you’ll gain: ✅Clarity on Definitions: What truly distinguishes orthosteric from allosteric
- 📰 GPCR Weekly News - January 9 to 15, 2023
Mandibulofacial dysostosis with alopecia results from gain-of-ETAR function via allosteric effects on
- Why Opposing Processes Matter for Your Next GPCR Drug
In this session, you’ll gain: ✅ A mental model you can trust for predicting how GPCR ligands behave
- 📰 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
- From DNA day to GPCR genomics
The G-protein-coupled receptors in the human genome form five main families.
- 📰 GPCR Weekly News, September 25 to October 1, 2023
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