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with chemist Johannes Broichhagen aka JB, the goal was bold and elegant: Create a photo-switchable ligand Hodson: physiology, disease context, and imaging logic JB: chemistry, ligand engineering, mechanistic Collaboration, Chemistry, and the Pivot That Changed the Project Goal:  Develop a photo-switchable GPCR ligand Result:  The switching didn’t work Observation:  Binding + localization were unexpectedly robust

September 5th to 26th, 2024 Registrants will learn: Essentials of measuring pharmacologic activity of ligands Application of this knowledge to determine the mechanism of action of new GPCR ligands. New ligands and new GPCR behaviors that produce unique drug profiles (i.e., intracellular ligands and opportunity to connect with like-minded scientists and researchers and gain valuable insights into the latest developments receptor subtypes Structural insights into ligand recognition, selectivity, and activation of bombesin

December 2022 Sosei Heptares Enters Antibody Discovery Agreement with Twist Bioscience to Discover and Develop (“the Company”; TSE: 4565), the world leader in GPCR-focused structure-based drug design (SBDD) and development , and Twist Bioscience Corporation (Nasdaq: TWST), a company enabling customers to succeed through its

This lesson helps you reframe how you interpret allosteric interactions —not as simple ligand displacement If your project involves GPCRs , functional selectivity , or non-traditional ligands , this session is In This Session, You’ll Gain: ✅ A clear explanation of why allosteric modulators don’t displace ligands—they allosteric cube The Allosteric Shift: When Receptors Become Something New In orthosteric pharmacology, a ligand No matter how much non-radioactive ligand you add, the binding curve levels off —because the receptor

Allostery isn’t just an advanced concept—it’s essential to understanding efficacy, ligand bias, and receptor As the GPCR field surges forward—from ligand bias to signaling diversity—the guest editors Dr. Why you need to be there: Learn how kinetic nuance shapes ligand design.   Access peer insights on allosteric modulators and biased ligands. If you work on GPCRs across translational pharmacology, drug development, or molecular pharmacology,

November 2021 Twist Bioscience Launches Revelar Biotherapeutics to Develop and Commercialize Novel COVID Executive Leadership Team Established with Demonstrated Success in Clinical, Regulatory and Commercial Development --(BUSINESS WIRE)--Nov. 15, 2021-- Twist Bioscience Corporation (NASDAQ: TWST), a company enabling customers has launched Revelar Biotherapeutics, Inc., an independently operated, new biotechnology company to develop

June 2022 "We’re delighted to welcome Dr Ed Brennan as our new Vice President, Head of Clinical Development Dr Brennan has extensive experience across all phases of clinical development, and across multiple therapeutic

Over time, she developed a fascination with how molecules influence biology and how that chemistry could The academic group Maria worked with had developed a technology that allowed for flexible, fast synthesis of fluorescent ligands. GPCR, is helping researchers worldwide gain access to customized, reliable assay tools without the delays and frustrations that often plague probe development. 👉 Learn more about Celtarys’ science-driven solutions

both homodimers and heterodimers, which may play a crucial role in modulating receptor function and ligand These dimeric interactions may contribute to the phenomenon of biased agonism, where ligands produce that disrupting the dimerization of GLP-1R results in decreased high-affinity binding to its natural ligand insight not only enhances our understanding of class B1 GPCR biology but also opens new avenues for developing Harikumar, K.G., et al., Impact of secretin receptor homo-dimerization on natural ligand binding.  

At a molecular level, different ligands bind to the same receptor and vice-versa (Marcuzzi et al. 2018 Drug discovery is shifting towards the development of biased ligands, which promote the engagement of and signaling patterns, by modulating ligand binding, as well as G-protein coupling or interaction with differences in the chemokine systems between species which, in some cases, hampers the pre-clinical development , unlike most of the class A GPCRs ligands that are small molecules or short peptides.

GPCR-targeting nanobodies. · Septerna: closed a $100 Million USD Series A round to develop small Developing Small Protein Therapeutics with a Novel Discovery Platform One way to overcome the challenges Orion used its discovery platform technology to rapidly develop a murinized version of OB-004 that was , and Orion has developed a unique and powerful solution to the problem, based on using the natural ligands Relevant Publications Development of Orion’s platform technology Hartley, O. et al. (2004) Proceedings

Predictive GPCR-Ligand Modeling Carlsson's work quickly shifted from curiosity to impact. Using virtual screening, he was able to identify novel ligands that aligned with experimental findings Rather than focusing solely on explaining receptor behavior post hoc, his group began developing workflows His lab has already begun using AlphaFold models to identify ligands for targets that lack experimental As predictive modeling matures, its role will continue to expand, guiding ligand discovery, informing

private group Certificate of participation Learn the essentials: Measuring the pharmacologic activity of ligands (affinity, efficacy, co-operativity) Determining mechanisms of action for new GPCR ligands Elements and effective GPCR discovery Master advanced applications: Using new cellular assays to analyze GPCR ligand behavior Predicting activity and in vivo target coverage with real-time kinetics Discovering new ligands

assumption about how your molecule behaves in a living system can sink months of work and millions in development In this session, you’ll gain: ✅ A mental model you can trust  for predicting how GPCR ligands behave Every ligand you design enters a system that is already balancing opposing forces—vasoconstriction vs You’ll come away asking Which of my ligands might be producing hidden signaling from inside the cell—and Ligands come and go, feedback loops kick in, and what you see in vitro rarely tells the whole story.

Study of small molecule binding to live cells provides important information on the characterization of ligands Here we developed and validated a label-free, liquid chromatography-mass spectrometry (LC-MS) based cell coupled receptor (GPCR), we used one antagonist as probe and multiple other antagonists as competitor ligands Competition binding analysis by titration of five known ligands suggested a good correlation with their This versatile method allows quantitative characterization of ligand binding to cell surface expressed

The advent of AlphaFold2 (AF2) has brought AI applications in drug development to unprecedented heights with atomic-level accuracy and remarkable scalability, providing crucial structural insights for drug development Despite its transformative potential, AI in drug development faces several challenges. Looking ahead, AI offers significant advantages in drug development, such as the ability to tackle complex AlphaFold2 structures guide prospective ligand discovery.

epidermal growth factor-induced phosphorylation of Gαi at specific residues predominantly inhibits ligand-induced Key findings include: Phosphorylation Hotspots: P Loop (Ser44, Ser47, Thr48): Impairs ligand-stimulated Interdomain Cleft (Ser151, Tyr154, Tyr155): Phosphorylation at Tyr154 and Tyr155 impaired ligand-stimulated C Terminus (Tyr320): Phosphorylation at Tyr320 disrupted Gβγ binding, receptor coupling, and ligand-stimulated This knowledge could inform the development of therapeutic strategies aimed at targeting specific phosphorylation

Hannes Schihada and his lab team developed fluorescent analogues for real-time binding studies of orphan Cloning and deorphanization of three inotocin (insect oxytocin/vasopressin-like) receptors and their ligand signalling molecule to exert direct functional effects in primary cultures of osteoblasts and osteoclasts Development Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating NEW Post-Doctoral Associate NEW Team Leader Antibody Discovery Staff Scientist (AC-TAP) in Database Development

Calculations "Allosteric modulators are called promising candidates in G protein-coupled receptor (GPCR) drug development receptor-lipid interface represent an uncharacteristic binding location that raises many questions about the ligand Although ligand-lipid interactions are weak, lipid tails play a role in ligand binding pose stability We discuss physicochemical aspects of ligand binding at the receptor-lipid interface and suggest a compound library enriched by weak donor groups for ligand search in such sites."

Visualizing GLP-1 & GIP Receptors in Islets and Brain Understanding incretin biology depends on more than ligand David Hodson walks through how his team uses fluorescence tools and chemically engineered ligands to Fluorescent ligand engineering clarifies receptor behavior that cell lines can’t reveal. Aside from his vast experience in drug development, not to mention his extensive publication record,

5 to 26, 2024 What You’ll Learn during the four sessions: How to measure pharmacologic activity of ligands (affinity, efficacy, co-operativity) Determining mechanisms of action for new GPCR ligands Key elements behavior Predicting activity and in vivo target coverage with real-time kinetics Discovering new ligands GPCRs and mRNA antigens enable drug discovery and development Mapping GPCR-RAMP complexes with MolBoolean GPR75 Modulators Using Medium-Throughput Reporter Gene Assay GPCR Therapeutics Optimizes the Joint Development

Historically, ligands for GPCRs have been identified before their receptor counterparts. , several unidentified receptors have been found and were labelled as “orphan” for their endogenous ligands shown to play key roles in various physiological functions, such as sensory perception, reproduction, development In addition, several GPR84 ligands have been described as well as GPR84 knockout mice. From these series of compounds, GLPG1205 progressed into clinical development for the potential treatment

CRCM Must-read publications : AlphaFold3 benchmarking for GPCRs; new structural insights into peptide ligand At first glance, when a ligand binds at two different affinities in the same system, it seems logical conditions, what appears to be a second high-affinity site may simply reflect kinetic factors—such as ligand-receptor-G structure-activity relationship (SAR) cycles Wasted optimization efforts Focus on leads that fail later in development Wendy Young : Career insights and lessons from a leader in drug development and a champion for women

the Gαi3 heterotrimers Activation/Deactivation Free-Energy Profiles for the β2-Adrenergic Receptor: Ligand is essential for meiosis and ascosporogenesis in the wheat scab fungus GPCR Binders, Drugs, and more Development of Photoswitchable Tethered Ligands that Target the µ-Opioid Receptor Design and Synthesis of Novel Meeting February 3 - 7, 2024 | SLAS2024 International Conference and Exhibition March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

Industry insights:  New alliances, pipeline shifts, and platform tech that could reshape metabolic drug development From cAMP to femtomolar ligands, she unpacks a career at the edge of precision signaling. Insights: • Receptor Localization Matters : Protein complexes pre-assemble at membranes, altering how ligands trigger responses. • Assay Development Gets Real : Fluorescent tools and real-world biology don’t always University access are coming—grandfather pricing ends in 2026. • Inclusive Growth : More access for developing

Discover how receptors actually behave, how ligands uniquely sculpt their function, and how cryptic allosteric

Application of computational methods for class A GPCR Ligand discovery. Methods & Updates in GPCR Research GPCRLigNet: rapid screening for GPCR active ligands using machine Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. Computational drug design postdoc at the Department of Drug Design and Pharmacology Software / database development PhD student at Department of Drug Design and Pharmacology Software / database development postdoc at

Propranolol with GPC-100 Sosei Heptares to Host R&D Day Highlighting its Innovative R&D and Late-Stage Development Progress Parker Moss to Join Exscientia as EVP, Corporate Development Confo Therapeutics Nominated for Meeting February 3 - 7, 2024 | SLAS2024 International Conference and Exhibition March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating Exhibition June 2 - 7, 2024 | Chemotactic Cytokines GPCR Jobs NEW Staff Scientist (AC-TAP) in Database Development

more nuanced, and mastering drug binding kinetics is essential for pipeline efficiency: How fast a ligand Competitive conditions —such as the presence of endogenous ligands— change kinetic behavior , and ignoring How do competing ligands slow or alter binding rates, and what does this tell you about real-world pharmacology

the immune system ORs are expressed in different blood cells where aroma compounds from butter, known ligands In the GI tract OR ligands drive an intracellular cascade that results in enhanced serotonin release Odorants, the natural ligands, could potentially be used as ligands and particular forms of odorant delivery The development of antibodies directed towards an OR could either drive receptor inactivation or activation , characterization of the function of ORs in vivo, development of in vitro systems for functional assays