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commercialization of novel medicines for patients with central nervous system (CNS) disorders, today announced the addition

November 2021 "Chronic use of most opioids causes tolerance; the new compounds avoid this and other unwanted qualities. November 22, 2021 JUPITER, FL—Scientists at Scripps Research in Florida have created a collection of new pain-relieving compounds that, like morphine and other drugs, provide relief via activation of opioid receptors, but without inducing many dangerous and unwanted side-effects that have driven opioid-related overdose and deaths." Read more at the source #DrGPCR #GPCR #IndustryNews

Juvenile Patient with Autism Spectrum Disorder with a Novel Combination of Copy Number Variants in ADGRL3 boy presenting both with autism spectrum disorder (ASD) and attention deficit/hyperactivity disorder (ADHD One of the CNVs is located on chromosome 4q13.1 in the region of the gene encoding for adhesion G protein-coupled receptor L3 (ADGRL3, former name: latrophilin-3, LPHN3), the other on chromosome 3p26.3 in the region To our knowledge, this is the first report of a CNV in the ADGRL3 gene and its first association with

the effects of RH on metabolic pathways associated with glucose counterregulation within liver, white adipose Methods: Using a widely adopted rodent model of 3-day recurrent hypoglycemia, we first checked expression Then, we examined epinephrine-induced phosphorylation of PKA substrates to validate adrenergic sensitivity Additionally, we measured circulating FFA and glycerol to check lipolysis.

We selected the adenosine receptor 2B (A2BAR), specifically expressed in cancer cell lines compared with

Few therapeutic agents have shown benefits when administered alone, but a few more have demonstrated clear improvement when administered in combination with other therapeutic molecules. In 2008 (and for the first time in the clinic), the therapeutic benefits of the β-adrenergic receptor This review highlights the clinical trials in which propranolol is taking part as adjuvant therapy at single administration or in combinatorial human trials, arising as a good pick and roll partner in anticancer

Applying Allosteric Modulator Pharmacology to Treat Dyskinesia and Other Movement Disorders with Tim Dyer Addex Therapeutics "Tim Dyer is the Co-Founder and CEO of Addex Therapeutics, which is focusing on the pharmacology Addex did not invent allosteric modulation but is pioneering the screening technologies to find these

#IPO #biotech #innovation #traitements #addiction #cannabis #Trisomie21 #Downsyndrome" Read more at the

mechanosensation-dependent behavior in C. elegans via a trans function Latrophilins are highly conserved Adhesion

outcomes on islet function that the altered GPCR expression status confers and the possible impact that adipokines

September 2022 "G protein‐coupled receptors (GPCRs) are valuable therapeutic targets for many diseases. A central question of GPCR drug discovery is to understand what determines the agonism or antagonism of ligands that bind them. Ligands exert their action via the interactions in the ligand binding pocket. We hypothesized that there is a common set of receptor interactions made by ligands of diverse structures that mediate their action and that among a large dataset of different ligands, the functionally important interactions will be over‐represented. We computationally docked ~2700 known β2AR ligands to multiple β2AR structures, generating ca 75 000 docking poses and predicted all atomic interactions between the receptor and the ligand. We used machine learning (ML) techniques to identify specific interactions that correlate with the agonist or antagonist activity of these ligands. We demonstrate with the application of ML methods that it is possible to identify the key interactions associated with agonism or antagonism of ligands. The most representative interactions for agonist ligands involve K972.68×67, F194ECL2, S2035.42×43, S2045.43×44, S2075.46×641, H2966.58×58, and K3057.32×31. Meanwhile, the antagonist ligands made interactions with W2866.48×48 and Y3167.43×42, both residues considered to be important in GPCR activation. The interpretation of ML analysis in human understandable form allowed us to construct an exquisitely detailed structure‐activity relationship that identifies small changes to the ligands that invert their pharmacological activity and thus helps to guide the drug discovery process. This approach can be readily applied to any drug target." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Several G-protein coupled receptors (GPCR) are upregulated in Alzheimer's Disease (AD), Yet, despite this upregulation, associated physiological effects are not observed in AD patients. paradox solicits urgent attention to find a suitable justification for disturbed neurotransmission in AD the role of Aβ granules and their possible interaction with GPCRs that modulate neurotransmission and AD

New ideas are added on top of existing ones. Complexity feels like progress. but learning slows down. 👉 This pattern usually shows up in a very specific way: 1️⃣ Experiments are added Additional data feels like risk reduction, even when it does not change the strategic picture. Instead of adding more work to feel safer, teams start designing fewer experiments with sharper intent They make uncertainty explicit rather than hiding it behind optimism or additional experiments. ✅ They

one’s aligned. 2️⃣ Founder-team decision asymmetry 👉 The founders make strategic calls in 1:1s or ad And now your next raise is behind schedule. 3️⃣ Strategic dilution 👉 You keep adding just one more It’s a leverage tool. ✅ When you fix alignment, you free up speed, clarity, and execution, without adding You adapt quicker without losing direction. . ✅ Science doesn’t just advance. It connects to business outcomes.

Although GPCRs are implicated in the pathophysiology of Alzheimer's disease (AD), biased GPCR signaling is a largely unexplored area of investigation in AD. and leads to a decrease in the area and compaction of amyloid plaques in the preclinical AppNL-G-F AD suggest a protective glial response that may limit amyloid plaque development in G protein-biased GPR3 AD the development of safer GPCR-targeting therapeutics with more directed pharmacological action for AD

protein-coupled receptor (GPCR) kinases (GRKs) are associated with the pathophysiology of Alzheimer's disease (AD However, GRKs have not been directly implicated in regulation of the amyloid-β (Aβ) pathogenic cascade in AD

This collaboration aims to amplify the visibility and adoption of Celtarys’ cutting-edge fluorescent ligand-receptor interactions, visualize binding in live cells, and design better experiments, core to advancing “This partnership will help accelerate the adoption of our chemical tools and foster collaborations that re excited to support the GPCR community with tools that deliver clarity, sensitivity, and speed,”  added GPCR empowers scientists and companies advancing receptor biology and drug discovery.

Pancreatic ductal adenocarcinoma, β-blockers and antihistamines: A clinical trial is needed Jillian G Özcan ,   Jimmy Caroli ,   Albert J Kooistra ,   David E Gloriam ,   Alexander S Hauser GPCRdb in 2025: adding GPCR Drug Discovery February 15 - 19, 2025 | BPS 2025 February 16 - 21, 2025 | Harnessing the Power of Advanced GPCR Photo-BQCA: Positive Allosteric Modulators Enabling Optical Control of the M1 Receptor The cell adhesion Updates in GPCR Research PGxDB: an interactive web-platform for pharmacogenomics research GPCRdb in 2025: adding

We've got 11 GPCR papers, seven industry news pieces, a new GPCR event, and even a job ad.   activity-modifying proteins Nicholas Kapolka , Geoffrey Taghon , and Daniel Isom  for their research on Advances mechanisms of action for new GPCR ligands Elements of a comprehensive and effective GPCR discovery Master advanced Reviews, GPCRs, and more G protein-coupled receptor (GPCR) gene variants and human genetic disease Advances Unprecedented fragment-based screening using Spectral Shift for GPCRs October 23 - 25, 2024 | 11th Adhesion

Registrations are closed but you can send an email to gpcrretreat@uottawa.ca to be added to the waitlist using a nanoscale hCCR3 receptor sensor GPCRs in Oncology and Immunology Phase 1/2 study of sorafenib added Use Disorder Reproducibility of Tanso Biosciences' GPCR Assay Septerna: making another run on GPCRs Addex Kevin Wright Joins GPCR Therapeutics as Director of Targeted and Immuno-oncology Sosei Heptares Adds World-leading Expertise to its Scientific Advisory Board Call for GPCR Papers opnMe GPCR Route 66+ project

But in allosteric systems , adding a modulator doesn’t push another molecule off—it transforms the receptor No matter how much non-radioactive ligand you add, the binding curve levels off —because the receptor Add G protein. Suddenly, the agonist works .

The Three-Layer Anti-Isolation Framework Breaking scientific isolation isn’t about adding more process

Antagonist “hogs” the receptor, depressing the response, even if more agonist is added.

Since then, Celniker has helped usher in an additional fund and headed a few startups as interim CEO. Adding it all up, Third Rock has raised $3.8 billion since its inception.

Allostery isn’t just an advanced concept—it’s essential to understanding efficacy, ligand bias, and receptor Terry Kenakin on “The Kinetics of Allostery: The Added Benefits of Allosteric Function.” across translational pharmacology, drug development, or molecular pharmacology, this is your decision advantage

To address this, he co-founded Superluminal Medicines , a biotech company focused on integrating machine In August 2025, Superluminal Medicines announced a collaboration with Eli Lilly and Company to advance From his early career redirection to startup setbacks, each step has added new layers to his thinking Advice for Young Scientists For early-career researchers, Ajay’s journey offers a powerful blueprint. Whether it's chronic pain, addiction, or another unmet need, keeping the real-world impact in focus can

Why Allosteric Modulators Expand Your Toolkit Allosterics offer a broader range of effects—additive, point, when a partial agonist is competing with endogenous tone, and when an allosteric modulator is adding

example, signal spontaneously, meaning a neutral antagonist won’t suppress appetite; it just blocks added

affect receptors’ properties.[10,11] BBVs also lack downstream signaling components, which can be an advantage The reaction was initiated by the addition of 1 μL D3 receptor displaying BBVs (CD3R = 0.7 nM) to 0.5 An equivalent volume of assay buffer was added to association controls (filled dark blue circles). The results suggest that adding the linker to the pharmacophore slows down both association and dissociation HEK293-D3R cells in DMEM medium with added 9% FBS and antibiotic antimycotic solution were incubated

You add a non-radioactive analog of a ligand, expecting it to displace binding. With a model, it becomes explainable: if the dimer form has higher affinity, then adding ligand actually Internal checks (like requiring a Schild regression slope of unity for competitive antagonism) add further Action” now Only in Terry’s Corner   Why Terry’s Corner When early choices determine which programs advance Subscriber-driven topics,  so the next lesson addresses your bottleneck.