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Lecture 4: Allosteric Modulators: NAMs, PAMs, Special Properties, Methods to quantify the allosteric effect

Lecture 3: Agonists and Efficacy: A New World of GPCR Efficacies / Biased Signaling

Lecture 2: Drug Affinity: Measurement of Antagonism (Binding and Function) / Classifying Antagonists

Lecture 1: GPCR Project Initiation and Design for Discovery of New Molecules

Class 4 - New dimensions of activity: Allosteric modulators and kinetics

Class 3 - Antagonist pharmacology and binding assay analysis

Class 2 - Quantifying agonist pharmacology and biased agonism

Class 1 - Concentration-response analysis: Become a CRC super-user

Class 4 - Characterizing Allosteric Modulators

Class 3 - Characterizing Antagonists

Class 2 - Characterizing Agonists

Class 1 - Fundamentals of Pharmacology

Gz-Enhanced Signal Transduction assaY (GzESTY) for GPCR deorphanization

Molecular determinants of ligand efficacy and potency in GPCR signaling

Panel Discussion on Publishing in Academia

Location bias of GRKs and Arrestins

Agonist bias at the Adenosine A1 Receptor: The story of BnOCPA

Ligand-biased signalling and location bias; two faces of functional selectivity

Accurate Mechanistic Calculation of μ Opioid Receptor Signaling Efficacy - Poster Presentation

Neuropeptide recognition and GPCR activation using the expanded receptor repertoire of nematodes – Insights into molecular signatures in vivo

Roundtable Discussion

Prevalence of pharmacologically active autoantibodies in heart failure, with dual action on serotoninergic 5-HT4 and muscarinic M2 receptors

Using small protein analogs to target challenging GPCRs

The Good, the Bad, and the Ugly

The Serotonergic Psychedelic N, N-Dipropyltryptamine Prevents Seizures in a Mouse Model of Fragile X Syndrome

Development of Functionally Selective Neurotensin Receptor 1 Ligands for the Treatment of Addiction

GRK2 Kinases in the Primary Cilium Initiate SMOOTHENED-PKA Signaling in the Hedgehog Cascade

Dual Targeting of GPCRs as a Therapeutic Approach

The ConfoBody® Technology: an efficient platform towards generation of GPCR agonistic antibodies

Functional modulation of PTH1R activation and signaling by RAMP2

Potentiation of ß-adrenergic receptor signaling by cell swelling

Ligand and G Protein Selectivity in Kappa Opioid Receptor

Structural basis of the regulation of human chemokine receptor and HIV-1 co-receptor CCR5

Career Panel

Biased Signaling Atlas & GPCRdb

Cannabidiol (CBD) decreases the hallucinogenic-like effects of lysergic acid diethylamide (LSD) via negative allosteric modulation of the serotonin 2A receptor

Animal toxins and GPCR, a promising combination for science and medicine

Dissecting structural determinants of GINIP required to modulate neurotransmitter GPCR signaling

GPR19 as a potential modulator of the aging process

Nanobody tethering of ligands to GPCRs promotes highly biased agonism

Biasing GPCR signaling by Ubiquitination

β-Adrenergic receptor signaling from the inner nuclear membrane

Activation Mechanism of Metabotropic Glutamate Receptor 5

Investigating Pluridimensional Signaling of Vasoactive G Coupled Protein Receptors

Chemokine receptor activation and signaling

Multiplexed selectivity screening of anti-GPCR antibodies

Early-stage development of an in vitro screening assay to characterize the activation of human adhesion receptor ADGRE5

Unconventional GPCR-PKA Signaling in the Hedgehog Pathway

PIP2-stimulated positive feedback drives Dishevelled recruitment to Frizzled GPCRs

Fantastic Adhesion GPCRs and How to Target them

Molecular and structural characterisation of GPR52, a novel target for schizophrenia

Towards the structure-based design of modulators of odorant GPCRs

Understudied GPCRs: Challenges and Opportunities

Understanding Orphan G Protein-Coupled Receptors and the enigmatic GPR146

Insights into the function of the orphan receptor GPR84

Adhesion GPCRs Latrophilins Orchestrate The Hierarchical Encoding of Cell Adhesion Cues to Dictate Context-Dependent Cell Functions: Implications for Neurological Disorders and Cancer

Wnt-stimulation induces conformational dynamics in the FZD-DVL complex

Translating the force - Mechano-sensing GPCRs

Integrating signaling kinetics into GPCR compound profiling

A Synaptic Adhesion Sensing Code Dictated by aGPCRs Latrophilins

High throughput GPCR screening technologies enable deciphering host-microbiome communication and the development of drug candidates

The cannabinoid CB1 receptor interacts with AT2 receptor. Expression of AT2-CB1 receptor heteromers in striatal neurons.

Spatiotemporal Signalling and Location of Fractalkine Receptor Cx3cr1 And Its Natural Genetic Variants Associated to Disease CX3CR1-V249I/T2

Relation between GPCRs, fibrosis and collagen in pancreatic tumors of KPC mice

Anti-inflammatory drugs for the treatment of neuroinflammation in Glaucoma

Location Bias of G Protein-Coupled Receptor Kinases Promotes Biased Signaling at CXCR3

The Interplay of Incretin Receptor Trafficking and Signaling in Pancreatic Islets

New GPCRdb structure and ligand resources

Neomorphic mutations in GNAO1 encephalopathy: from mechanisms to drug discovery

Regulation of Metabotropic Glutamate Receptor Signaling: Role in Huntington’s and Alzheimer's Diseases

Modeling of CCR2 homodimers and CCR5/CCR2 heterodimers

A1 receptor and CB1 receptor heteromeric interaction. Expression and signalling in primary cultures and CPZ model tissue samples.

Structure-guided GPCR drug discovery: Focus on psychedelics

Exploration of GPCR signaling using nanobody-ligand conjugates

Application of optical GPCR & G protein biosensors for drug discovery & assessment of constitutive activity

Environment Matters: One Receptor but many targets

Biased Allosteric Modulators in Drug Discovery

A new machine learning based method for ADRB2 agonist detection using single-ligand dynamic interaction data

Solvation affects the conformational dynamics of GPCRs

Role of constitutive Gq signalling from endosomes by US28 in glioblastoma

Mechanism of Activation of a Family B GPCR

Isolating ligand binding kinetics of mini G protein bound GPCR receptor conformations

Disentangling autoproteolytic cleavage from tethered agonist-dependent activation of the adhesion receptor ADGRL3

Regulation of Expression of CB2-5HT1A receptor complexes by cannabinoids in animal models of hypoxia and in oxygen-glucose deprived cells.

GPCR-mediated regulation of aging-related disease

The Electrostatic Switch: a new model for CCR5 desensitization based on dynamic modulation of negative charges at the receptor-ligand interface

Experimental and computational analysis of biased agonism on full-length and a C-terminally truncated adenosine A2A receptor

Virtual Reality in GPCR Structure-based Drug Design: The Orexin System and Suvorexant

Functional modulation of PTH1R activation and signaling by RAMP2

Cancer-associated GAIN domain somatic mutations reduce cell signaling and motility of Lphn3 functions

A Journey of discovery with CCR5: from basic science to the clinic via new technology

Explainability approaches - solution to the machine-learning-based assistance in compounds optimization

GPCR fragment-based drug discovery enabled by the Confo Therapeutics technology

Getting the most from your biosensor assays: Data analysis for GPCR discovery

Oxytocin-Vasopressin Ligand-Receptor Bias

Targeting muscarinic receptors to slow neurodegenerative disease

Enabling the discovery of next generation therapeutics via the ebBRET-based biosensor technology bioSensAll

Fine-tuning glutamate receptor activity with allosteric modulators for neurodegenerative and psychiatric disorders

Molecular mechanism of formation of GPCR domains at the cell surface

Exploring circuit selective GPCR functions using intersectional Crispr/Cas9 approaches

Welcome to the Ecosystem

ArcoScreen a new GPCR screening platform

GPCR activation mechanisms across classes and macro/micro scales

Twist Biopharma: Synthetic DNA Technologies Enable Fast and Responsive anti-GPCR Antibody Discovery and Optimization

Structure and dynamics of GPCRs: lessons from cryo-EM

“Better Medicine, One Assay at a Time” Save time, energy, and cost from Target to IND

Designer G protein-coupled receptors as tools to identify novel targets for antidiabetic and anti-obesity drugs

GPCRomics: Identifying novel GPCR targets in health and disease

A Funny Thing Happened at the Dr. GPCR Summit

Structure-guided drug discovery

Nanobody tethering to dissect GPCR pharmacology

Celtarys Research: Innovative Chemistry to Illuminate Biology

Advancing GPCR drug discovery with bioSensAll® platform technology

The challenges of targeting RXFP1, the receptor for the heart failure drug candidate relaxin, with peptide mimetics and small molecules

Construction of GPCR heteromer database and validation of CXCR4-GPCRx heteromers

Healing is a matter of time

Heat Shock Protein 90 is a Novel Opioid Receptor Signaling Regulator that can be Targeted to Improve Opioid Therapy

Engineering a human GPCR to create self-tunable engineered yeast probiotics for the treatment of inflammatory bowel disease

CXCR4 heteromers as novel cancer targets

A general method for quantifying ligand binding to unmodified receptors using Gaussia luciferase

A distinct activation mechanism in GPCR dimers: Insights from cryo-EM snapshots of the entire Class D1 GPCR activation pathway

Assessing Serotonin 1A Receptor Expression and Function in Adult Fmr1 Knockout Mice, a Preclinical Model of Fragile X Syndrome

FR900359: nature’s weapon and treasure trove for basic and translational research

Chaperoning G protein-coupled receptors

The Phosphorylation Barcode as a Mechanism of Biased β-arrestin 2 Recruitment and Conformation at CXCR3

GPCRdb Resources

Unconventional GPCR Signaling in the Hedgehog Pathway

Innate Proximity: Utilizing the Inherent Physicality of Receptor Interactions for Drug Development

Molecular basis of adhesion GPCR activation

Where a Ph.D. Can Lead

Hydroxycarboxylic acid receptor 3 and GPR84 signaling with potential implications for immune cell function

Toolboxing solid-state NMR spectroscopy for GPCR studies

Marginal phenotypes with orphan GPCRs: a GPR37L1 case study

Through the Looking-Glass: Structure-Based Drug Discovery across the GPCRome

Integrating computational modeling and experimental data to unravel the molecular and intracellular effects of a disease-linked variant of the oxytocin receptor

Phosphorylation of the M1 muscarinic acetylcholine receptor protects from neurodegenerative disease

Profiling of GPCR complexes

Applying structure-based ligand design to low-resolution GPCR structures

Follicle-stimulating hormone induces lipid droplets via Gai and beta-arrestin in an endometrial cancer cell line

Nanobody tethering to explore GPCR pharmacology

Free energy calculations reveal key aspects of GPCR modulation

The metabolic relevance of adhesion G protein-coupled receptors

The molecular basis for high-affinity agonist binding at the beta1-adrenoceptor

An aripiprazole analog with two binding modes at the dopamine D2 receptor

Noncanonical scaffolding of Gαi and β-arrestin by G protein-coupled receptors

Making the most of your Ph.D. and postdoc – building career relevant skills

Identification of PDZ‐RhoGEF as a novel target of Gαi

Bitter taste GPCRs and their ligands

Cryo-EM structure of human GABA(B) receptor

Sweet taste of heavy water is mediated by taste GPCR receptor

Orphan receptor GPR139 inhibits mu-opioid receptor signaling through activation of Gq/11

Molecular pharmacology of cannabinoids: beyond THC

Tracking dopamine D1 receptor signaling in Parkinsonian and dyskinetic rats with FRET biosensors and fiber photometry

Heat shock protein 90 is a novel regulator of opioid signal transduction in brain and spinal cord

Finding the sweet spot: modeling of the sweet taste receptor and discovery of sweet compounds

The economic realities of lab automation to maximize productivity and improve reproducibility

Operant self-stimulation of thalamic terminals in the dorsomedial striatum is constrained by metabotropic glutamate receptor 2

Nuclear beta-1 adrenergic receptors mediate rapid norepinephrine-induced PKA responses in astrocytes

The GPCR database, GPCRdb

Fluorescent biosensors for GPCR signaling kinetics

Multiplexed analysis of the secretin-like GPCR-RAMP interactome by suspension bead array

Analyzing kinetic signaling data for GPCRs: Straightforward curve fitting methods for time-course data

Molecular insights into the signalling of CLR:RAMP complexes

Role of water and lipids in G-Protein-Coupled Receptor rhodopsin activation

The phosphorylation barcode in biased chemokine signaling

Interactions between Gβγ and RNA polymerase II regulate transcription in cardiac fibroblasts

Bitopic ligands for cannabinoid CB2 receptors

Dr. GPCR Summit Networking Event

Discovery of novel antagonists of NPFF receptors 1 and 2 from in silico screening

Novel pairings in the human peptide-receptor signaling system

Unraveling G protein-coupled receptor activity in women’s health

Cell Signaling by Protease-activated Receptors

The canonical and non-canonical function of β-arrestins in adipose tissue metabolism

Adhesion GPCRs: Cis and trans-signaling shape communication in cell polarity and division

GBCRdb for beginners

Automated micro-plate-based methods for quantifying GPCR activation

The role of ubiquitin in GPCR signaling and trafficking

New Resources in GPCRdb

Illuminating the druggable GPCR-ome

Time is your enemy, GPCRs are your friend

All About Addgene - More Open and Reproducible Science with Materials Sharing

Quantifying the kinetics of GPCR signaling

Dr. GPCR Ecosystem: From idea to the community

Identification of GPCRs Modulating Flow-induced Signaling Pathways in Vascular Endothelial Cells

New structural perspectives in G protein-coupled receptor-mediated Src family kinase activation

The Impact of Anionic Lipids on GPCR Function and Conformational Dynamics

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