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  • 📰 GPCR Buzz: August 5-11, 2024 | Top Highlights from DrGPCR University!

      Postdoctoral Position Postdoctoral research position Senior or Lead Researcher   Senior Scientist, Cryo-Electron

  • Dr. GPCR University registration is now open! Secure your spot now!

    Postdoctoral Position NEW Postdoctoral research position Senior or Lead Researcher Senior Scientist, Cryo-Electron

  • Embark on a GPCR Adventure: Your Weekly Research Expedition! | Oct 21-27, 2024

    Embark on another exciting exploration of the unknown realms of GPCR research. Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and

  • Unlocking the Future of Medicine: Advancements in GPCR Research

    Congress of Basic and Clinical Pharmacology GPCR Jobs NEW Senior or Lead Researcher NEW Senior Scientist, Cryo-Electron

  • Dynamic recognition of naloxone, morphine and endomorphin1 in the same pocket of µ-opioid receptors

    The endogenous peptide ligand endomorphin-1 (EM-1) underwent almost no significant conformational changes To validate these processes, we employed GIRK4S143T, a MOR-activated Gβγ-protein effector, in combination key residue I322, which leads to differential recognition of morphine and naloxone while assisting EM inhibitor directly into an agonist of MOR, and I322A also significantly attenuated the potency of MOR on EM

  • From GPCR Data Chaos to Decisive Action

    I call it the Lego Bucket Problem : You’ve got CRO output, internal assay data, maybe even some promising Data arrives too fast and too fragmented CROs deliver output without clear integration Teams chase the This is embedded consulting for biotech and VC teams who need to move fast —without compromising scientific True Embedded Partnership I review CRO scopes, flag risks early, and sit in on your strategic calls. Who I Work With ✅ Biotech Teams  – Especially those lacking in-house GPCR leads or overwhelmed by CRO

  • Although the cannabinoid type-2 receptor (CB2) is highly expressed in the immune system, emerging...

    September 2022 Cannabinoid type-2 receptors: An emerging target for regulating schizophrenia-relevant circuits "Although the cannabinoid type-2 receptor (CB2) is highly expressed in the immune system, emerging

  • Septerna emerges with $100M to spark 'second golden age' of prolific drug target GPCR with ...

    February 2022 Septerna emerges with $100M to spark 'second golden age' of prolific drug target GPCR with

  • Research Network on Signal Transduction (ERNEST) has established an Emergency Fund for Ukrainian ...

    March 2022 ERNEST has established an Emergency Fund for Ukrainian researchers.

  • Karuna Therapeutics Announces Positive Results from Phase 3 EMERGENT-2 Trial of KarXT in...

    August 2022 Karuna Therapeutics Announces Positive Results from Phase 3 EMERGENT-2 Trial of KarXT in psychiatric and neurological conditions, today announced positive topline results from its Phase 3 EMERGENT

  • Accelerating GPCR Drug Discovery

    The assays are running, data is flowing in from your CROs or your internal labs , yet progress stalls So, I created a new path—one that allows me to embed, optimize, and accelerate GPCR programs from the Internal data and CRO outputs  misaligned with strategic goals. Embedded Execution:  I work alongside your team—not above it. Collaborative Partnership:  I embed, contribute, and build solutions hand-in-hand with your team.

  • Breaking the Myth of High and Low Affinity Sites

    Kenakin’s Emerging Drug Hunter  lecture delivers exclusive, cutting-edge insights that help you move Terry's Corner _____ #GPCR #BindingAffinity #Pharmacology #DrugDiscovery #LeadOptimization #TerryKenakin #EmergingDrugHunter

  • Your GPCR Program Decisions Depend on Good Data Interpretation

    But Terry Kenakin’s new Emerging Drug Hunter lecture reveals why this assumption can mislead even experienced an in vitro pharmacology group from scratch—not just a lab, but a culture that encouraged curiosity, empowered on Terry’s Corner  digital pharmacology courses Priority access to insights from major conferences, emerging Hashtags: #GPCR #DrGPCR #BindingAffinity #Pharmacology #DrugDiscovery #LeadOptimization #TerryKenakin #EmergingDrugHunter

  • Why Kinetics Matter More Than Kd in GPCR Drug Discovery

    Identify emerging targets:  Allosteric modulators, biased ligands, and kinetic frameworks will dominate on Terry’s Corner  digital pharmacology courses Priority access to insights from major conferences, emerging Hashtags: #GPCR #DrGPCR #BindingAffinity #Pharmacology #DrugDiscovery #LeadOptimization #TerryKenakin #EmergingDrugHunter

  • Accelerating GPCR Drug Discovery: What 40 Years of Pharmacology Reveal

    the sooner you know whether anything’s happening—and whether it’s the right or wrong thing,” Kenakin emphasizes CRO partnerships are essential for most discovery programs, but they often break down on communication CROs have standard ways of doing them. You must bridge that gap,” Kenakin notes. How to embrace (not fear) allosteric complexity. How better CRO communication prevents costly errors. 👉  Join Terry’s Corner & Secure Your Spot for the

  • Emerging approaches for decoding neuropeptide transmission

    November 2022 "Neuropeptides produce robust effects on behavior across species, and recent research has benefited from advances in high-resolution techniques to investigate peptidergic transmission and expression throughout the brain in model systems. Neuropeptides exhibit distinct characteristics which includes their post-translational processing, release from dense core vesicles, and ability to activate G-protein-coupled receptors (GPCRs). These complex properties have driven the need for development of specialized tools that can sense neuropeptide expression, cell activity, and release. Current research has focused on isolating when and how neuropeptide transmission occurs, as well as the conditions in which neuropeptides directly mediate physiological and adaptive behavioral states. Here we describe the current technological landscape in which the field is operating to decode key questions regarding these dynamic neuromodulators." Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

  • Beyond the Probe: Scaling Innovation From the Bench to Product Launch

    It’s empathy. Maria emphasizes the importance of genuinely listening to researchers: understanding the biological question Whether supporting CROs, academic labs, or pharma teams, Celtarys engages deeply with collaborators to

  • Chronic itch: emerging treatments following new research concepts

    Until recently, itch pathophysiology was poorly understood and treatments were poorly effective in relieving itch. Current progress in our knowledge of the itch processing, the numerous mediators and receptors involved has led to a large variety of possible therapeutic pathways. Currently, inhibitors of IL-31, IL-4/13, NK1 receptors, opioids and cannabinoids, JAK, PDE4 or TRP are the main compounds involved in clinical trials. However, many new targets, such as Mas-related GPCRs and unexpected new pathways need to be also explored. Read full article

  • A Note from Yamina: Building the Next Chapter of Dr. GPCR

    Science Meets Execution The Foundry is where we bring together biotech innovators, Venture Capital, CRO And coming early next year: the CRO Bank , connecting GPCR-focused companies and teams with trusted contract They go beyond sponsorship to bring tools and technologies directly to the researchers who use them , empowering Our Ambassador Program empowers community members to share Dr. You can always reach me at hello@DrGPCR.org  — and yes, we read every email.

  • Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on Inflammation..

    However, in epithelial cells, OGR1 promotes epithelial to mesenchymal transition (EMT) and inflammation

  • Molecular creativity in drug discovery

    Must-read publications:  Emerging targets, signaling dynamics, and acid-sensing receptors in disease. : • The Foundry Arrives : R&D meets biotech with real-world acceleration, strategic consulting, and CRO

  • The development of modulators for lysophosphatidic acid receptors: A comprehensive review

    ), and one radioligand (BMT-136088/18F-BMS-986327) has entered phase Ⅰ clinical trials for positron emission

  • How GPCR Collaboration Built an Innovation Engine

    What emerged wasn’t just another pharmacology group — it became a collaborative engine for GPCR discovery receptor assays PhD students trained across multiple techniques, not just one pipeline Senior scientists embedded Biotech teams, CRO alliances, and academic consortia face the same challenge: how to align incentives

  • Is Your GPCR Drug Discovery Program Built for Breakthroughs or Breakdowns?

    I understand that embracing a systematic approach can feel daunting, especially with the pressure to actionable guide for implementing this holistic approach within your own GPCR operational strategy , emphasizing I work with biotechs, VCs, and CROs to implement the framework that ensures every step forward is strategic

  • Understanding the Journey: Catherine Demery's Path to Addiction Science

    Learning the Lab, Learning Herself During her time at the contract research organization (CRO) in Ann Embracing Change and Uncertainty Change can be daunting, especially when it involves stepping away from However, embracing uncertainty can lead to unexpected opportunities.

  • A robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.

    provide unique advantages as donors, since they have extended fluorescence duration, enable delayed emission readings, have narrow bands and high stokes shift, which prevent cross-excitation and cross-emission In this case, CELT-335 exhibits exc and em at 650nm and 673nm, which are compatible with the lanthanide In the saturation experiments, specific binding was also checked, employing appropriate competitors ( Cannabinoid Receptor Type 1 in Parkinson’s Disease: A Positron Emission Tomography Study with [ 18 F  

  • Using Live-cell High-Content Screening to Characterize CB2 Ligands: Insights From 16 Synthetic Cannabinoids

    The cannabinoid receptor type 2 (CB2R) has emerged as a compelling target across inflammation, immune Among 16 SCRAs evaluated, three compounds—AAN396, AAN397, and AAN405—emerged as nanomolar binders with

  • How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology

    For JB, that moment was a cold email from a biologist he’d never met, asking if he could synthesize a Transformed GPCR Imaging and Outperformed Antibodies As JB continued exploring the biology, a major obstacle emerged JB emphasizes how much of their progress came from staying open, asking questions freely, and engaging

  • How to Avoid the Most Common Gaps in Your Biotech Pitch

    But without concrete context, they’re empty. Your listener doesn’t want to be impressed.

  • GPCR Pharmacology Insights That Prevent Real Drug Discovery Failures

    synthesize the key topics addressed during the AMA and highlight the GPCR pharmacology insights that emerged Its clinical utility emerged from the interplay between β₁-mediated inotropy and α-mediated vascular Kenakin  emphasized that the key advantage is not subtlety for its own sake—it’s bounded pharmacology EC₅₀ and Emax uncouple affinity and efficacy, making cross-agonist comparison unreliable. Dr. Kenakin  emphasized that only operational-model–derived ratios anchored to a benchmark partial agonist

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