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involved in a wide array of physiological and disease functions, yet knowledge of their role in colon cancer reveal that PAR-induced post-transcriptional regulation of β-catenin is centrally involved in colon cancer

targets for drug discovery, however, their role in oncology is underappreciated and GPCR-based anti-cancer identified GPR108, a GPCR protein described in innate immune system, is a potential therapeutic target of cancer Depletion of GPR108 dramatically inhibited the survival of various cancers. Overall, our findings supported GPR108 as a promising therapeutic target of cancer, and provided a small molecule inhibitor GA directly and selectively targeting GPR108 for cancer therapy."

August 2022 "Chemokines, a subgroup of cytokines along with their receptors, are involved in various biologic processes and regulation of a wide range of immune responses in different physiologic and pathologic states such as tissue repair, infection, and inflammation. C-X-C motif chemokine receptor 4 (CXCR4), a G-protein-coupled receptor (GPCR), has one identified natural ligand termed stromal-derived factor-1(SDF-1 or CXCL12). Evidence demonstrated that the ligation of SDF-1 to CXCR4 initiates several intracellular signaling pathways, regulating cell proliferation, survival, chemotaxis, migration, angiogenesis, adhesion, as well as bone marrow (BM)-resident cells homing and mobilization. Additionally, CXCR4 is expressed by tumor cells in blood malignancies and solid tumors." Read more at the source #DrGPCR #GPCR #IndustryNews

Drug discovery and development: Role of basic biological research. Biomedical researchers' perspectives on the reproducibility of research. G Protein-Coupled Receptors: A Century of Research and Discovery. The paradox from within: research participants doing-being-observed. Qualitative Research. 2015;16(4):446-467. 56.         Wilner W.

Elizabeth Johnstone were awarded one of the 2022 Diabetes Research Grants at the World Diabetes Day Breakfast Perkins Professor Kevin Pfleger and Dr Elizabeth Johnstone who were awarded one of the 2022 Diabetes Research This $60,000 grant from Diabetes Research WA will assist the Perkins' Molecular Endocrinology and Pharmacology

October 2022 Identification of A2BAR as a potential target in colorectal cancer using novel fluorescent targeted in a wide range of diseases, but few therapies have been directed against GPCRs in the field of cancer Here, using colorectal cancer (CRC) as a model, we explored the gene expression of a panel of GPCRs in We selected the adenosine receptor 2B (A2BAR), specifically expressed in cancer cell lines compared with

August 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer physiological processes, these activities are also involved in the onset and progression of various cancers primary emphasis on the signaling processes which underlie the mechanism of β-arrestins in the onset of cancer processes has important implications for understanding the therapeutic intervention and treatment of cancer

September 2022 Fentanyl activates ovarian cancer and alleviates chemotherapy-induced toxicity via opioid receptor-dependent activation of EGFR "Background Fentanyl is an opioid analgesic and is widely used in ovarian cancer Although increasing evidence has suggested the direct role of fentanyl on cancer, little is known on the effect of fentanyl on ovarian cancer cells. Methods Proliferation, migration and apoptosis assays were performed in ovarian cancer cells after fentanyl

Tackling the GPCR Imprecision Problem: Strategic Planning for Sustainable Progress in Complex Systems. In the high-stakes world of GPCR drug discovery , breakthrough science isn't enough. You can have the most brilliant minds and cutting-edge assays, but if your science isn't continuously integrated with your GPCR operational strategy and investment goals, even the most promising program can falter. This fundamental disconnect between the lab and the boardroom  is precisely where programs get stuck—not because of bad science, but because companies find themselves throwing more money and people at problems that could be solved with better systems. This reactive approach, driven by a "go fast" mindset, burns through precious capital and time, leaving both scientific teams and investors frustrated. Companies find themselves throwing more money and people at problems that could be solved with better systems . This reactive approach, driven by the prevailing wisdom of "going fast" and focusing only on the science, burns through precious capital and time, leaving both scientific teams and investors frustrated. This belief that we don't have time to build better systems is a costly miscalculation. It reminds me of a conversation I recently overheard: my oldest child complaining about having to do 'everything at the same time ,' only for the youngest to wisely respond, 'No, you just need to do one thing at a time .' This simple truth applies profoundly to the "go fast" culture in biotech. We believe we don't have time to build better systems, but in reality, our most brilliant and expensive minds are stuck with low-impact tasks due to a lack of systems thinking . My perspective on this challenge is shaped not by a 40-year journey at the bench, but by an expertise in systems thinking  and operational discipline . My work isn't just  about the latest and best assay; it's about the framework that ensures the right assay data leads to the right decision. This is the critical piece that often gets lost in the "go fast" culture—the integration of science with strategy and flawless execution. I’ve lived this firsthand, not just in theory, but by building these systems from the ground up. I understand that embracing a systematic approach can feel daunting, especially with the pressure to move quickly. At Dr. GPCR, we recognized this core problem. Our Chief Brainstorm Officer, Attila Foris , is building a system so transparent that anyone joining the company can integrate seamlessly. Every time a problem arises, we trace it back to its root cause, implementing changes that prevent its recurrence. This iterative process of continuous, planned improvement ensures you're always addressing the next critical area. This is the essence of de-risking GPCR programs through operational excellence. This kind of continuous improvement doesn't happen organically; it demands intentional planning and a systematic approach, ensuring every step forward is strategic and sustainable. The Role of Systems Thinking in GPCR Drug Discovery Systems thinking is the intentional practice of seeing the entire GPCR program as a single, interconnected entity. It's the opposite of a reactive approach, where problems are solved in isolation. It’s the fundamental framework for building your Precision Blueprint , ensuring every scientific detail, operational process, and strategic decision aligns to create a seamless, predictable pathway to success. What You'll Learn in This Series Over the next five bi-weekly installments, " The GPCR Precision Blueprint " series will unpack how to bridge this critical gap. I'll show you how to transform your drug discovery process from a series of disconnected efforts into a seamless, predictable, and de-risked pathway. Part 1: The GPCR Imprecision Problem : I'll reveal why reliance on hiring more people over investing in robust systems thinking  is a multi-million dollar mistake. We'll look at how overlooked operational details, such as misaligned data from diverse GPCR assay types or communication gaps in cross-functional collaboration , lead to critical costs. Part 2: The Data Disconnect : Discover how fragmented, unmanaged GPCR data  cripples scientific progress and strategic decision-making. Learn how to build an integrated data pipeline  that transforms this chaos into a strategic asset. Part 3: The Financial Friction : Explore how a lack of precise alignment between GPCR scientific milestones  and financial realities creates significant risk. Learn to tie your program's progress directly to your funding runway, incorporating crucial early commercial and medical foresight. Part 4: The Investor Imperative : Understand what investors truly prioritize beyond just great science. Learn to translate your program’s internal operational precision into a compelling, de-risked narrative  that builds confidence and secures critical venture capital . Part 5: Your Precision Blueprint : I'll tie it all together, providing a concise, actionable guide for implementing this holistic approach within your own GPCR operational strategy , emphasizing that precision is a continuous, intentional journey towards predictable success. The GPCR Precision Blueprint is more than a concept. If you're ready to move beyond the articles and build these systems for your own GPCR program, let's connect. I work with biotechs, VCs, and CROs to implement the framework that ensures every step forward is strategic and sustainable, offering precision scientific and operational guidance  to accelerate discovery . 🚀 Book your free 30-minute strategy call Let’s unlock the momentum your GPCR program needs. 👉 https://calendly.com/drgpcr/yamina-corner Or explore how we can work together: 👉 Yamina.org

October 2022 "Single-molecule counting techniques enable a precise determination of the intracellular abundance and stoichiometry of proteins and macromolecular complexes. These details are often challenging to quantitatively assess yet are essential for our understanding of cellular function. Consider G-protein-coupled receptors-an expansive class of transmembrane signaling proteins that participate in many vital physiological functions making them a popular target for drug development. While early evidence for the role of oligomerization in receptor signaling came from ensemble biochemical and biophysical assays, innovations in single-molecule measurements are now driving a paradigm shift in our understanding of its relevance. Here, we review recent developments in single-molecule counting with a focus on photobleaching step counting and the emerging technique of quantitative single-molecule localization microscopy-with a particular emphasis on the potential for these techniques to advance our understanding of the role of oligomerization in G-protein-coupled receptor signaling." Read more at the source #DrGPCR #GPCR #IndustryNews

the Formation of a Scientific Advisory Board comprising international leaders in GPCRs pharmacology, immunology

September 2022 "Background Cancer driver genes are usually ranked by mutation frequency, which does not with few driver mutations overall, because these few mutations should be strong enough to initiate cancer

November 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer physiological processes, these activities are also involved in the onset and progression of various cancers primary emphasis on the signaling processes which underlie the mechanism of β-arrestins in the onset of cancer processes has important implications for understanding the therapeutic intervention and treatment of cancer

September 2022 Lack of Oestrogen Receptor Expression in Breast Cancer Cells Does Not Correlate with Kisspeptin Signalling and Migration "Kisspeptin is an anti-metastatic mediator in many cancer types, acting through However, controversy remains regarding its role in breast cancer since both pro- and anti-metastatic In KISS1R overexpressing triple-negative breast cancer (TNBC) cells, stimulation has been associated

August 2022 Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based kinetic studies "G protein-coupled receptors (GPCRs) are an important receptor superfamily and common therapeutic targets. The second messenger cyclic adenosine monophosphate (cAMP) is a key mediator in many GPCR signaling pathways. Monitoring intracellular cAMP levels can help identify orthosteric agonists and antagonists, as well as allosteric modulators. In this regard, luminescence-based biosensors have revolutionized our ability to monitor GPCR signaling kinetics. The GloSensor™ cAMP assay enables real-time monitoring of signaling downstream of many GPCRs. However, it is crucial to optimize assay conditions such as temperature. As well, it has not been reported whether the effects of temperature on biosensor activity are reversible. Here, we describe the temperature sensitivity and reversibility of the GloSensor™ cAMP assay, and which GloSensor™ version is optimal for measuring cytosolic cAMP. We also present a detailed protocol for monitoring cAMP levels in live cells expressing endogenous or exogenous GPCRs. Temperature optimization studies were carried out using HEK293H cells transiently transfected with the adenosine receptor A2a and the GloSensor™ plasmid (pGloSensor-20F or -22F). We found that preincubation and luminescence reading at room temperature were optimal as compared to higher temperatures. As well, the GloSensor-22F biosensor had a superior signal-to-background ratio and the effect of temperature on biosensor activity was reversible. However, thermal instability of the biosensor may pose a problem for in vivo studies. Nevertheless, the GloSensor™ cAMP assay can be applied to analyze signaling by a wide range of GPCRs for drug discovery" Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer adenocarcinoma (PDAC) remains an aggressive disease that is expected to become the second cause of cancer -mediated knockdown of YES1 and transfection of epitogue-tagged YAP mutants in PANC-1 and MiaPaCa-2 cancer

Exploring Intracellular Targets: Bridging the Gap Between In Vitro and In Vivo GPCR Research - August and a research associate/scientist in in vitro pharmacology. GPCR Podcast : The Future of GPCR Drug Discovery with Molecular Modeling The field of GPCR research is research within the field of Cellular Biochemistry. Discover the research topic ➤ Why Dr.

September 2022 Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on Here, we report that the Ovarian Cancer G-Protein Coupled Receptor1 (OGR1 or GPR68) has dual roles in

The Tools to Detect Them Using the multiplexed GPCR library and Luminex assay , researchers can now: is being bound Determine if the antibody is activating or inhibitory Guide diagnostics or treatment research This is the future of GPCR immunology . ________________ Keyword Cloud : GPCR autoantibodies , GPCR immunology

Upregulated in Hepatocellular Carcinoma "Hepatocellular carcinoma (HCC) is at the forefront of the global cancer , with some members of the RGS family being associated with liver cancer as well. Considering this, we investigated the role of RGS20 as a potential prognostic marker in 28 different cancer By using the Cancer Genome Atlas (TCGA) and Gene Expression Omnibus (GEO) data, our analysis revealed Our analysis further supports the putative function of RGS proteins, particularly RGS20, in cancer."

October 2022 Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected Here, we revealed that dimerization of β2-AR is responsible for the constitutive activity of β2-AR generating

However, the role of β2-AR in oral cancer is not well identified.

Here, we revealed that dimerization of β2-AR is responsible for the constitutive activity of β2-AR generating

Embark on this week’s thrilling updates in GPCR research, learning opportunities, and industry developments Innovate UK announced the winners of its Transforming Cancer Therapeutics grant, which focuses on developing life-changing cancer treatments. circuitries in mouse visual cortex by a single G protein-coupled receptor type (5-HT2A) GPCRs in Oncology and Immunology power of many: Multilevel targeting of representative chemokine and metabolite GPCRs in personalized cancer

Miles Thompson, Alexander Hauser, Caroline Gorvin et al. for their research on GPCR gene variants and endothelial to mesenchymal transition Role of pH-sensing receptors in colitis GPCRs in Oncology and Immunology Polarizing itch Biochemical pharmacology of adenylyl cyclases in cancer Methods & Updates in GPCR Research protein-coupled receptor (GPCR) gene variants and human genetic disease Advances and challenges in cancer Inflammatory Bowel Disease (IBD) Domain Therapeutics and Chime Biologics Form Manufacturing Pact for Antibody Cancer

The sheer complexity of the cell and the astonishing diversity of diseases are just two reasons why researchers For example, chemotherapy, a powerful standard approach to kill fast-growing cancer cells, has the drawback Nevertheless, researchers have a host of new technologies at their disposal to develop targeted therapies Modern drug development approaches include a range of techniques leveraging structural biology, immunology

GPCR Symposium for the year, focusing on GPCRs in Immunology and Oncology, concluding the Dr. Between Two Sibling Nematode Species: Bursaphelenchus xylophilus and B. mucronatus GPCRs in Oncology and Immunology pathway network and its dynamics in the mesenchymal transition of glioblastoma Methods & Updates in GPCR Research TRUQAP™ (capivasertib) plus fulvestrant approved in the US for patients with advanced HR-positive breast cancer Associate I, Tissue Culture Post-Doc Research Associate Postdoctoral Fellow Research Scientist/Postdoctoral

Towards the convergent therapeutic potential of GPCRs in autism spectrum disorders GPCRs in Oncology and Immunology Molecular characterization of breast cancer cell pools with normal or reduced ability to respond to 2023 Half Year And Second Quarter Financial Results And Provides Corporate Update Sosei Heptares and Cancer Research UK Announce the Dosing of the First Patient in a Phase I/IIa Trial with Cancer Immunotherapy Laboratory Specialist Associate NEW Postdoc Research Associate Director, Regulatory Affairs Research

of attention because of its involvement in various diseases, such as idiopathic pulmonary fibrosis, cancers

Regulator of G protein signaling 16 restrains apoptosis in colorectal cancer through disrupting TRAF6 Metallo-protease Peptidase M84 from Bacillusaltitudinis induces ROS-dependent apoptosis in ovarian cancer receptor-related gene signature through bioinformatics analysis to construct a risk model for ovarian cancer mitochondria and reprograms fungal cells for nematode hunting Role and recent progress of P2Y12 receptor in cancer and Discovery Challenges and opportunities in cancer immunotherapy: a Society for Immunotherapy of Cancer