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But in Melbourne, a quiet experiment challenged that model — and it worked. Funding models rewarded independence, not shared resources. Engineering Collaboration: The Monash Lab Model Traditional academic labs mirror feudal structures. The Monash model flipped that logic: Shared infrastructure, not duplicated equipment Centralized core What Changed After This Data The pooled funding model turned the lab into a magnet: postdocs, visiting

Dopamine D2 receptor modulators  – transforming treatment for Parkinson’s & schizophrenia. Allosteric modulation  for unprecedented precision. Serotonin & dopamine receptor modulation  for neuropsychiatric disorders. These sessions bridge structural biology , computational modeling , and clinical translation  — with

peptides designed from the intracellular loops of G protein-coupled receptors (GPCRs) that act in an allosteric manner to modulate the activity of GPCRs.

Addex Therapeutics Ltd (SIX: ADXN and Nasdaq: ADXN), a clinical-stage pharmaceutical company pioneering allosteric modulation-based drug discovery and development, today announced that it has entered into a definitive

Addex Therapeutics Ltd (SIX: ADXN and Nasdaq: ADXN), a clinical-stage pharmaceutical company pioneering allosteric modulation-based drug discovery and development, today announced that it has entered into a definitive

factor-dependent phosphorylation of Gαi shapes canonical signaling by G protein-coupled receptors Kinetic Model epithelial cells GPCR Binders, Drugs, and more Structure-based identification of a G protein-biased allosteric modulator of cannabinoid receptor CB1 GPCR function in autophagy control: a systematic approach of chemical Treg Depleting anti-CCR8 Antibodies, Including Best-in-class Candidate DT-7012 Crinetics Announces Positive Fellow—Pharmacology/Cell Biology/Biochemistry Post Doctoral Fellow Postdoc Position Join Dr.

By modulating receptor expression or sensitivity, we can shift the “lens” through which drug activity Model patient-like pathophysiological states (e.g., reduced receptor expression in heart failure). Adjusting assay sensitivity—whether through expression systems, chemical modulation, or engineered desensitization—provides What emerges is not just more data—it’s the right data, positioned to inform strategic decision-making If you’re still treating orthosteric and allosteric interactions as interchangeable, you’re leaving precision

Signaling Sonja Peter , Brian Bender , Chris De Graaf   for their excellent work on Comparative Study of Allosteric infection: IUPHAR Review 41 Structural and Molecular Insights into GPCR Function Comparative Study of Allosteric

We report that arrestin-3 modulates Fgr activity with a hallmark bell-shaped concentration-dependence interaction, we determined the crystal structure of the Fgr SH3 domain at 1.9 Å resolution and developed a model This model suggests that Fgr interacts with arrestin-3 at multiple sites and is consistent with the locations

A conserved intracellular allosteric binding site (IABS) has recently been identified at several G protein-coupled showing that our CCR9-PROTAC is able to reduce CCR9 levels, thereby offering an unprecedented approach to modulate

Monitoring intracellular cAMP levels can help identify orthosteric agonists and antagonists, as well as allosteric modulators.

disturbances GPCR Binders, Drugs, and more Gut microbe-generated phenylacetylglutamine is an endogenous allosteric modulator of β2-adrenergic receptors GPCRs in Neuroscience In-silico predicted mouse melanopsins with Caenorhabditis elegans Calcium-sensing receptor regulates Kv7 channels via Gi/o protein signalling and modulates antigens enable drug discovery and development Mapping GPCR-RAMP complexes with MolBoolean Screening GPR75 Modulators Postdoctoral research position Senior or Lead Researcher   Senior Scientist, Cryo-Electron Microscopy

agonism by Gαi/o-biased stapled peptide agonists of the relaxin-3 receptor GPCR kinases differentially modulate cannabinoid receptor agonists at the cannabinoid CB1 receptor Why classical receptor theory, which ignores allostery , can effectively measure the strength of an allosteric effect as agonist's efficacy GPCR Binders, Drugs Imaging Center Scientific Assistant Postdoctoral Fellowship- Mechanistic Biology Research Scientist Post-Doc position Join Dr.

Breakthroughs this week: C. elegans avoids EGCG via SRXA-7 GPCR; a bidirectional GPCR switch modulates immune signaling; a machine-learning tool predicts GPCR–ligand kinetics; and cryo-EM uncovers a new allosteric We kick off with a question that cuts deep: What if your models could actually predict the future? Jens Carlsson  (Uppsala University) joins Yamina  to explore how computational modeling is evolving from

Mandibulofacial dysostosis with alopecia results from gain-of-ETAR function via allosteric effects on GPCR Binders, Drugs, and more Modelling altered signalling of G-protein coupled receptors in inflamed GPCR Allostery: a View from Computational Biology.

From restricted tissue diffusion to PK–PD dissociation, Kenakin equips you with the kinetic models and In This Session, You’ll Gain: ✅ Modeling tools to understand how restricted diffusion  in tissues like window ✅ Examples of how rebinding in dense receptor environments  amplifies target occupancy, even post-clearance PK–PD Dissociation: When Clearance Doesn’t Mean It’s Over The lecture’s standout example: Aplaviroc, an allosteric Kenakin offers not just theory, but tools to model, predict, and validate this behavior early.

September 2022 "Metabotropic γ-aminobutyric acid receptor (GABABR), a class C G protein-coupled receptor (GPCR) heterodimer, plays a crucial role in the central nervous system. Cryo-electron microscopy studies revealed a drastic conformational change upon activation and a unique G protein (GP) binding mode. However, little is known about the mechanism for GP coupling and activation for class C GPCRs. Here, we use molecular metadynamics computations to predict the mechanism by which the inactive GP induces conformational changes in the GABABR transmembrane domain (TMD) to form an intermediate pre-activated state. We find that the inactive GP first interacts with TM3, which further leads to the TMD rearrangement and deeper insertion of the α5 helix that causes the Gα subunit to open, releasing GDP, and forming the experimentally observed activated structure. This mechanism provides fresh insights into the mechanistic details of class C GPCRs activation expected to be useful for designing selective agonists and antagonists." Read more at the source #DrGPCR #GPCR #IndustryNews

GPCR Binders, Drugs, and more Allosteric modulator potentiates β2AR agonist-promoted bronchoprotection in asthma models.

GPCR Symposium on ''GPCRs as Therapeutic Modalities' Share your project with a 1-minute abstract video involved in the innate immune response of Tribolium castaneum GPCR Activation and Signaling Biased allosteric Discovery On Target September 27 - 28, 2023 | Training Seminar "The Renaissance in GPCRs as Drug Targets: Allosteric

Career opportunities:  New openings for a postdoctoral research position in GPCR biochemistry and biophysics Avoid missed opportunities:  Discover how to identify and target cryptic intracellular allosteric sites GPCR Podcast : The Future of GPCR Drug Discovery with Molecular Modeling The field of GPCR research is Learn how his research aims to develop models that can distinguish between active and inactive ligands

Expression Ligand bias at the muscarinic acetylcholine receptor family: opportunities and challenges Modulating Structural and Molecular Insights into GPCR Function Vibrational Energy Landscapes and Energy Flow in GPCRs Allosterism Industry News Confo Therapeutics Announces EUR 60M Series B Financing to Advance a Pipeline of Novel GPCR-Modulating July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs NEW Postdoctoral Position NEW Postdoctoral research position Senior or Lead Researcher Senior Scientist, Cryo-Electron Microscopy

5th to 11th, 2024 GPCR Activation and Signaling Constitutive activation mechanism of a class C GPCR Allosteric modulation and G-protein selectivity of the Ca2+-sensing receptor GPCRs in Cardiology, Endocrinology Research GPCR-BERT: Interpreting Sequential Design of G Protein-Coupled Receptors Using Protein Language Models Imaging Center NEW Scientific Assistant Postdoctoral Fellowship- Mechanistic Biology Research Scientist Post-Doc position Lead Researcher Join Dr.

Statin-induced increase in actin polymerization modulates GPCR dynamics and compartmentalization. The G protein-coupled receptor neuropeptide receptor-15 modulates larval development via the transforming Stabilization of pre-existing neurotensin receptor conformational states by β-arrestin-1 and the biased allosteric modulator ML314. Scientist II DOE (Native Mass Spectrometry) Senior Vice President of Global Medical Affairs Postdoctoral Position

In particular, CBD is able to modulate different receptors in the endocannabinoid system, some of which While in the former, CBD has been demonstrated to function as an antagonist, the way by which CBD modulates suggested to directly trigger receptor’s activation, stabilize CB1 inactive conformations or function as an allosteric modulator. These results are in agreement with the proposed modulatory function of each ligand, showing that the

of polycystic ovarian syndrome by modulating GPCR41/43 and PROKR1 GPCRs in Neuroscience Diverse signaling prologue Industry News Exscientia Business Update for Third Quarter 2023 Addex CEO Tim Dyer to Discuss Allosteric Modulators in Neurological Disorders at Jefferies Healthcare Conference in London Sosei Heptares and NEW July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology 2026 GPCR Jobs NEW Post-Doc Postdoctoral Fellow Research Scientist/Postdoctoral Associate in Computational Chemistry/Biophysics Post-Doctoral

Breakthroughs this week: McGPCR multimodal model; Endocrine Metabolic GPCRs 2026; Pfizer–Metsera acquisition why misclassification propagates error across affinity estimates, mechanism claims, and downstream modeling Watch the trailer 👇 What you’ll gain Validate the model behind the data.   four canonical criteria to distinguish genuine orthosteric antagonism from apparent shifts that mask allosterism

3 activation Michael Trogdon, J Silvio Gutkind, Edward C Stites, et al., for their study on Systems modeling its Aldehyde from a Marine Cyanobacterium Fluorophore-Labeled Pyrrolones Targeting the Intracellular Allosteric beige adipocyte formation: Implications for obesity and metabolic health GPCRs in Neuroscience Chronic modulation treatment based on drug repurposing demonstrates mutation-agnostic efficacy in pre-clinical retinopathy models Cryo-Electron Microscopy Postdoctoral Research Associate Senior Scientist - Discovery Biotherapeutics Post-Doctoral

for their investigation on Modulation of contextual fear acquisition and extinction by acute and chronic internalization of cognate GPCRs and disrupt downstream intracellular signaling Therapeutic potential of allosteric modulators for the treatment of gastrointestinal motility disorders GPCRs in Cardiology, Endocrinology Neuroscience Neuron specific quantitation of Gαolf expression and signaling in murine brain tissue Modulation cortex Unveiling the therapeutic prospects of EGFR inhibition in rotenone-mediated parkinsonism in rats: Modulation

Brake for Airway Smooth Muscle Cell Movement Hepatic extracellular ATP/adenosine dynamics in zebrafish models Chemoattractant receptor signaling in humoral immunity Industry News Neurosterix launches with $63M to Advance Allosteric Modulator Therapeutics for Neurological Disorders Aelis Farma Reports Its 2023 Annual Financial Resultsand

Orthosteric and allosteric antagonists of C5aR1 are a novel strategy for anti-inflammatory therapies.