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Improves the Work Itself For JB, questions fuel the way he designs chemical probes, collaborates with biologists What limitation is biology solving? Throughout his own journey—from organic chemistry to chemical biology to GPCR imaging—every pivotal step

It became the center of gravity. It happened because the chemistry and the biology met in the right way. Realizing tissue is alive, unpredictable, and full of hidden structure. It gives scientists a way to feel the biology. Better GPCR imaging doesn’t just capture biology — it expands the biological questions the field can

Professor Charlotte Deane, Ph.D., of the University of Oxford, has joined Exscientia as Chief Scientist of Biologics focus on the application of artificial intelligence (AI), machine learning, and the design of protein structures She has held numerous senior roles at the University of Oxford, where she is currently Professor of Structural

binding by searching large-scale motions accompanied with stable maintenance of the fragile cell-membrane structure

Electron cryo-microscopy (cryo-EM) is a powerful technique for the structural characterization of biological macromolecules, enabling high-resolution analysis of targets once inaccessible to structural interrogation In recent years, pharmaceutical companies have begun to utilize cryo-EM for structure-based drug design Structural analysis of integral membrane proteins, which comprise a large proportion of druggable targets Structural characterization of biologics, such as vaccines, viral vectors, and gene therapy agents, has

that causes the Gα subunit to open, releasing GDP, and forming the experimentally observed activated structure

October 2022 Mechanism of enhanced sensitivity of mutated β-adrenergic-like octopamine receptor to amitraz in honeybee Apis mellifera: An insight from MD simulations "Background: Amitraz is one of the critical acaricides/insecticides for effective control of pest infestation of Varroa destructor mite, a devastating parasite of Apis mellifera, because of its low toxicity to honeybees. Previous assays verified that a typical G protein-coupled receptor, β-adrenergic-like octopamine receptor (Octβ2R), is the unique target of amitraz, but the honeybee Octβ2R resists to amitraz. However, the underlying molecular mechanism of the enhanced sensitivity or toxicity of amitraz to mutated honeybee Octβ2RE208V/I335T/I350V is not fully understood. Here, molecular dynamics simulations are employed to explore the implied mechanism of the enhanced sensitivity to amitraz in mutant honeybee Octβ2R." Read more at the source #DrGPCR #GPCR #IndustryNews

GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health physiological balance between healthy and pathological conditions; thus, their importance in systems biology

Indoles, benzodiazepines, phenethylamines — each recurs because it “fits” biology well.  It was early structure-based pharmacology. Dr. They are structural strategies for tuning physiology. therapeutic windows More predictable clinical behavior Allosteric modulation allows us to work with  biology Does it interact with the receptor in a way that biology can use?

GPCR empowers scientists and organizations advancing GPCR biology and GPCR-targeted drug discovery.

transducer of the hedgehog (HH) morphogen, which plays an essential role in the patterning of epithelial structures

G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular effector proteins. Different agonists can promote differential receptor-induced signaling responses - termed bias - potentially by eliciting different levels of recruitment of effector proteins. As activation and recruitment of effector proteins might influence each other, thorough analysis of bias is difficult. Here, we compared the efficacy of seven agonists to induce G protein, G protein-coupled receptor kinase 2 (GRK2), as well as arrestin3 binding to the muscarinic acetylcholine receptor M3 by utilizing FRET-based assays. In order to avoid interference between these interactions, we studied GRK2 binding in the presence of inhibitors of Gi and Gq proteins and analyzed arrestin3 binding to prestimulated M3 receptors to avoid differences in receptor phosphorylation influencing arrestin recruitment. We measured substantial differences in the agonist efficacies to induce M3R-arrestin3 versus M3R-GRK2 interaction. However, the rank order of the agonists for G protein- and GRK2-M3R interaction was the same, suggesting that G protein and GRK2 binding to M3R requires similar receptor conformations, whereas requirements for arrestin3 binding to M3R are distinct. Read full article

Career opportunities:  Discovery biology roles and training paths in GPCR signaling. But drugs aren’t just biology—they’re chemical matter. From opium to antibiotics, nature’s molecules still outperform many designed compounds. • The Power of Structure privileged scaffolds and rational design open the door to dual activity and precision. • Cheminformatics to Biologics altering how ligands trigger responses. • Assay Development Gets Real : Fluorescent tools and real-world biology

New structural tools, AI-driven design pipelines, and a growing number of programs moving into the clinic biotech and pharma to advance GPCR programmes from discovery through translation — experts in GPCR biology , structural biology, computational design, pharmacology, and translational strategy. Will Barnes is Executive Director and Head of GPCR Biology at Iambic Therapeutics, where he leads AI-driven structural modeling for GPCR drug discovery.

For over two decades, my work has centered on GPCR pharmacology . I was always the one identifying what could be improved: The essential structure that was missing. But without structure, it's just a messy pile of colored blocks. My Approach: Biology, Execution, Systems My consulting approach uniquely blends deep pharmacology expertise Here's how I bring a fresh perspective: Biology-First, Data-Driven Strategy:  I help you focus on the

Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs Scientist I Cell Biology Hauser Group Postdoctoral Scholar – iPSC in cardiac and endothelial cell function Protein Biochemist/Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry Postdoc in GPCR mechanosensing   Biology and Drug Discovery Approaches Altered PLCβ/IP3/Ca2+ Signaling Pathway Activated by GPRCs in

year, with no plateau INAUGURATION OF AELIS FARMA NEW LABORATORY at Institut Européen de Chimie et Biologie Keys to Medical Therapies From Structure to Solution: How Structural Biology Informs the Development Congress of Basic and Clinical Pharmacology GPCR Jobs NEW GPCR Molecular Pharmacologist Scientist - Biology Scientist I Cell Biology - Tectonic Therapeutic Senior Principal Scientist, Medicinal Chemistry PhD Biologist GPCR Activation and Signaling Exploring Bias in GPCR Signaling and its Implication in Drug

April 2022 Ono Enters into Collaboration Agreement with Domain Therapeutics and Université de Montréal

16 session on iPSC-derived translational models, and a new podcast episode with Joseph Kim on GPCR structural biology and drug discovery at opioid and galanin receptors. limitation when signaling outcomes depend on cell type, signaling complex assembly, and disease biology Joseph Kim: Structural Biology and Drug Discovery at GPCRs Cryo-EM has transformed how we visualize receptor–ligand In this episode, Joseph Kim, a postdoctoral scholar in Ashish Manglik's lab at UCSF, discusses structural

They fail because the interpretation of that data did not translate to biology outside the assay system Biology reveals targets. Key realities pharmacologists face: Assays measure one slice of biology Disease physiology involves many mechanistic insight into receptor signaling quantitative frameworks for decision making Chemists contribute: structural Even promising molecules collapse due to safety issues, pharmacokinetics, or unexpected biology.

March 2022 "Explicyte grants Domain Therapeutics exclusivity on data related to GPCR implicated in immunoresistance, to develop first-in class innovative cancer therapies. Strasbourg and Bordeaux, France, March 10, 2022 – Domain Therapeutics, a biopharmaceutical company specializing in the discovery and development of new drugs targeting G Protein-Coupled Receptors (GPCRs) in immuno-oncology (IO), and Explicyte, an expert in the field of IO and innovative target identification through multiparametric approaches, announce today the signing of a partnership agreement. The two companies will combine their expertise to identify GPCR targets and associated biomarkers to discover and develop breakthrough therapeutic programs for IO. Financial terms are not disclosed." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered agonist-mediated activation mechanism "The mechanistic details of the tethered agonist mode of activation for the adhesion GPCR ADGRF5/GPR116 have not been completely deciphered. We set out to investigate the physiological importance of autocatalytic cleavage upstream of the agonistic peptide sequence, an event necessary for NTF displacement and subsequent receptor activation. To examine this hypothesis, we characterized tethered agonist-mediated activation of GPR116 in vitro and in vivo. A knock-in mouse expressing a non-cleavable GPR116 mutant phenocopies the pulmonary phenotype of GPR116 knock-out mice, demonstrating that tethered agonist-mediated receptor activation is indispensable for function in vivo. Using site-directed mutagenesis and species-swapping approaches, we identified key conserved amino acids for GPR116 activation in the tethered agonist sequence and in extracellular loops 2/3 (ECL2/3). We further highlight residues in transmembrane 7 (TM7) that mediate stronger signaling in mouse versus human GPR116 and recapitulate these findings in a model supporting tethered agonist:ECL2 interactions for GPR116 activation." Read more at the source #DrGPCR #GPCR #IndustryNews

Nicholas Kapolka , Geoffrey Taghon , and Daniel Isom  for their research on Advances in yeast synthetic biology for human GPCR biology and pharmacology Dr. from October 23-25, 2024, to connect with fellow scientists and explore the latest in adhesion GPCR biology protein-coupled receptor (GPCR) gene variants and human genetic disease Advances in yeast synthetic biology for human G protein-coupled receptor biology and pharmacology Industry News Muscarinic drugs breathe

Biased signaling frameworks centered on receptor conformations have a structural limitation when selectivity Separately, signaling outputs derived from heterologous systems often fail to reflect the biological This session with Kenneth Jacobson and Matteo Pavan examines the structural determinants that make selective HEK293 systems are powerful tools for scalable pharmacological screening, but they have a structural limitation when signaling outcomes depend on cell type, signaling complex assembly, and disease biology

Georgios Skiniotis as Director of the New Center of Excellence for Structural Cell Biology Monash Scholars 2024 January 13 - 16, 2025 | PepTalk 2025 January 25 - 29, 2025 | SLAS 2025 February 15 - 16, 2025 | Structural July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs NEW Scientist - Biology Scientist I Cell Biology - Tectonic Therapeutic Senior Principal Scientist, Medicinal Chemistry PhD Biologist GPCR Activation and Signaling Beyond the classic GPCR: unraveling the role of GPR155 role

December 2022 Sosei Heptares Enters Antibody Discovery Agreement with Twist Bioscience to Discover and December 2021 – Sosei Group Corporation (“the Company”; TSE: 4565), the world leader in GPCR-focused structure-based

blockbuster weight-loss drugs Transforming Drug Discovery: Insights from Viva Biotech's GPCR and TPD Structural Biology Platforms GPCR Events, Meetings, and Webinars December 10 - 12, 2024 | Pharmacology 2024 January 13 - 16, 2025 | PepTalk 2025 January 25 - 29, 2025 | SLAS 2025 February 15 - 16, 2025 | Structural and World Congress of Basic and Clinical Pharmacology GPCR Jobs GPCR Molecular Pharmacologist Scientist - Biology Scientist I Cell Biology - Tectonic Therapeutic Senior Principal Scientist, Medicinal Chemistry PhD

to Solution: How Structural Biology Informs the Development of Drugs Targeting G Protein-Coupled Receptors Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs Scientist I Cell Biology Biologist Senior Scientist/Staff Scientist, Computational Chemistry GPCR Activation and Signaling A Biology and Drug Discovery Approaches Altered PLCβ/IP3/Ca2+ Signaling Pathway Activated by GPRCs in

May 2022 Sosei Heptares and Kallyope Enter Collaboration to Identify and Validate Novel Gastrointestinal will gain unique and valuable access to the Sosei Heptares compound library for its industry-leading biology company, and New York City-based Kallyope, pioneers in drug discovery involving the gut-brain axis, have entered

His career moved through veterinary school, immunology, neuroendocrinology, and finally into islet biology This collaboration reshaped the way Hodson’s lab studies receptor biology. Chemistry, imaging, physiology, and structure finally intersected. will hinge on the teams who can map GPCR signaling with precision and design therapies that fit real biology They’re team problems — the kind that require chemistry, physiology, pharmacology, structural biology