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- đ° GPCR Weekly News, February 27 to March 5, 2023
Keep in mind that you can always change your email preferences in your account settings. There is no limit to the number of posters we can accommodate, so hurry and submit your poster so that we can add it to the list of posters and increase the number of people who can ''stop by'' it on March
- Conservation of Allosteric Ligand Binding Sites in G-Protein Coupled Receptors
Mapping of Alphafold2 generated models of these proteins confirms that the same sites can be identified These sites cluster at nine distinct locations, and each can be found in many different proteins.
- đ° GPCR Weekly News, March 13 to 19, 2023
Remember, you can always adjust your email preferences in your account settings. For Dr. There is no limit to the number of posters we can accommodate, so hurry and submit your poster so that we can add it to the list of posters and increase the number of people who can ''stop by'' it tomorrow
- Purpose-Driven Opioid Research: Catherine Demeryâs Academic Path
Careers built on prestige, titles, or external pressure can burn out quickly. how opioids impair breathing, why xylazine complicates interventions, and how receptor-level insights can
- From One to Many: How a GPCR Curiosity Became a Field-Wide Toolkit
âThe beauty of multiplexing is that you can do many things with one pot of samples.â â Tom Sakmar Enter
- Nuclear localization of histamine receptor 2 in primary human lymphatic endothelial cells
imparts many unresolved questions, such as the functional relevance of this localization, and whether H2R can contribute directly to transcriptional regulation and can affect lymphatic specific gene expression.
- Transmembrane domains of GPCR dimers â a novel hot spot for drug discovery
Transmembrane domains of GPCR dimers â a novel hot spot for drug discovery G-protein-coupled receptors (GPCRs) can form biologically active homodimers or heterodimers which drive specific signaling pathways that can But how can we target GPCR dimers? Recent studies found that peptides derived from the transmembrane region of GPCRs can block the formation
- GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026
When these factors arenât understood, binding data can appear precise while quietly misleading decision-making Broichhagen, and David Hodson discuss GLP-1 receptor probes, fluorescence-based assays, and why availability can
- Dimerization of GPCRs: Novel insight into the role of FLNA and SSAs regulating SST2 and SST5...
and SSAs regulating SST2 and SST5 homo- and hetero-dimer formation "The process of GPCR dimerization can SST2 and SST5 can also form endogenous hetero-dimers in these cells. In conclusion, we demonstrated that in GH3 cells SST2 and SST5 can form both homo- and hetero-dimers
- đ° GPCR Weekly News, September 25 to October 1, 2023
Unfortunately, registration has closed, but you can still join the waitlist by emailing gpcrretreat@uottawa.ca You can submit your logo design by November 1st, and registration is unnecessary to participate. You can find all the necessary information on the Logo Contest page.
- Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5
excitatory neurotransmitter of the nervous central system, L-glutamate, and mGlu5 receptor activity can illustrate how access to high-resolution structures of GPCRs in complex with allosteric modulators can
- đ° GPCR Weekly News, September 18 to 24, 2023
If you couldn't make it, no sweat â our premium members can always go back and watch the recorded talks Registration is now closed, but you can join the waitlist by emailing gpcrretreat@uottawa.ca. Novo Nordisk's North Carolina semaglutide plant Excellerate Bioscience Announces Site Relocation AI can
- High-Content Screening for GPCR Programs: Overcoming Assay Limitations with Fluorescent Ligands
These challenges can obscure real biological signals and complicate the identification of robust hits Probe panelsâsuch as lysosomal dyes or cytoskeletal markersâcan be integrated to support multiplexed When combined with a competitor such as the CB2-selective partial agonist GW40583, displacement curves can
- Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5
excitatory neurotransmitter of the nervous central system, L-glutamate, and mGlu5 receptor activity can illustrate how access to high-resolution structures of GPCRs in complex with allosteric modulators can
- Chemical Drug Matter : Rethinking the Molecules We Choose to Develop In Drug Discovery
Does it interact with the receptor in a way that biology can use? Members can also propose new topics, ensuring relevance to real-world discovery problems.
- Dynamic GPCR activation revealed through time-resolved Cryo-EM
With this high-resolution, dynamic view of GPCR activation, scientists can better tackle diseases by Beyond GPCRs, the methods and insights from this study can be applied to other fast, transient biological
- When Pain Becomes a Catalyst: How Personal Experience Redefined One Scientistâs Mission
Alex Serafiniâs journey proves how personal pain can lead to professional purpose â and why the next
- Assay Volume Control: Your GPCR Drug Discovery Power Lever
Premium: Sneak Peek A fast editorial preview of what Premium Members get in full this week â so you can Itâs built to compress your time to clarityâso you can pick better targets, stress-test hypotheses earlier
- Luciferase-based GloSensorâą cAMP assay: Temperature optimization and application to cell-based kinet
Monitoring intracellular cAMP levels can help identify orthosteric agonists and antagonists, as well Nevertheless, the GloSensorâą cAMP assay can be applied to analyze signaling by a wide range of GPCRs
- The Five Traps of Ignoring Kinetics
Thatâs your signal: kinetics are moving faster than your tools can measure. lectures  that sharpen the tools you actually use in discovery A growing on-demand library  of lessons you can
- Join the #GPCR movement today!
Did you know that you can enjoy a Dr. GPCR Ecosystem paid membership with extra benefits?
- How a Failed Med School Dream Sparked a GPCR Biotech Revolution
Whether it's chronic pain, addiction, or another unmet need, keeping the real-world impact in focus can Itâs about how moments of redirection â even disappointment â can open new paths to impact.
- Signaling pathways activated by sea bass gonadotropin-inhibitory hormone peptides in COS-7 cells...
These data indicate that sea bass GnIHR signals can be transduced through the PKA and PKC pathways, and GnIH can interfere with kisspeptin actions by reducing its signaling.
- Enhanced membrane binding of oncogenic G protein αqQ209L confers resistance to inhibitor YM-254890
They can also function independently of GPCR activation upon acquiring mutations that prevent GTPase YM-254890 (YM) can inhibit signaling by both GPCR-activated wild type αq and GPCR-independent αqQ209L
- Mapping Motion: Intermediate States, Deorphanization & Discovery
challenge dogma and deepen our view of receptor dynamics, from the surprising discovery that ÎČ-arrestin can
- Building Backwards: Why Top-Down Models Could Revolutionize Pain Research
"I'm particularly interested in model development... seeing if we can bring preclinical models much closer
- đ° GPCR Weekly News, March 6 to 12, 2023
There is no limit to the number of posters we can accommodate, so hurry and submit your poster so that we can add it to the list of posters and increase the number of people who can ''stop by'' it on March
- New Tools, Smart Signals, and The Kenakin Brief
You can already explore the platform and subscribe to The Kenakin Briefâour new newsletter packed with
- First AMA of 2026: GPCR Pharmacology, Biased Signaling & Mechanistic Clarity
What seems definitive during early screening can shift as assay systems, receptor expression levels,
- Therapeutic validation of an orphan G proteinâcoupled receptor
orphan GPCR (Sharman et al., 2011), although it is widely accepted that mediumâchain fatty acids (MCFAs) can and 2. which ligands can be used as tool compounds to study the function and biology of this receptor distinct functional outcomes of agonist ligands (Pillaiyar et al., 2018) with biased properties which can















