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  • Exscientia welcomes Richard J. Law, as their new Chief Business Officer

    March 2022 "Congratulations to Richard J. Law, our newly named Chief Business Officer. Richard is the architect behind nearly all of Exscientia's partnerships and collaborations across pharma

  • Targeted Therapies to Reduce Side Effects in Modern Drug Development

    December 2021 "Drug development is rarely trivial. In fact, it is often costly, frustrating, and tortuous—and more often than not it ends in failure. The sheer complexity of the cell and the astonishing diversity of diseases are just two reasons why researchers typically require years to uncover the mechanisms of disease before they can even dare to contemplate the development of therapeutic options and begin the long, arduous road to the clinic. Drugs that do make it to clinical trials have major hurdles to clear—not the least of which is safety testing. It is necessary for drugs to evaluated for potential toxicities and side effects, and these key factors must be deemed tolerable before investigators can assess drug potency. For example, chemotherapy, a powerful standard approach to kill fast-growing cancer cells, has the drawback of causing damage to healthy cells in the process, leading to side effects that can include pain, nausea, and hair loss. Nevertheless, researchers have a host of new technologies at their disposal to develop targeted therapies that minimize side effects. Modern drug development approaches include a range of techniques leveraging structural biology, immunology, cell signaling, and more to address the challenge. As this article shows, progress is being made on multiple fronts." Read more at the source #DrGPCR #GPCR #IndustryNews

  • Angiotensin-(1-7) improves cognitive function and reduces inflammation in mice following mild trauma

    September 2022 Angiotensin-(1-7) improves cognitive function and reduces inflammation in mice following

  • Better GPCR Drug Discovery Decisions Start With Structured Learning

    Terry Kenakin at a significantly reduced cost. This is not commentary. It is structured access and structured education. Reduce external training spend while increasing scientific depth.

  • Ode to GPCRs

    GPCRs mediated signal transduction.[47] The 2000 Nobel Prize in Physiology or Medicine went to Eric Richard The 2004 Nobel Prize in Physiology or Medicine went to Richard Axel and Linda Brown Buck for their work Press release: The 2004 Nobel Prize in Physiology or Medicine to Richard Axel and Linda B. Richard Axel – Facts - NobelPrize.org. https://www.nobelprize.org/prizes/medicine/2004/axel/facts/. 61

  • Inside the New Dr. GPCR Ecosystem: Learning, Insight, and Momentum for 2026

    Clearer signals  — curated insights that reduce noise without oversimplifying complexity. Early assays prevent late failure  — modern in vitro tools dramatically reduce attrition . Your membership also supports open educational resources for the global GPCR community, ensuring depth

  • Identification and functional characterization of the sulfakinin and sulfakinin receptor in the...

    characterized SK and SKR genes in the D. armandi and carried out bioinformatics predictions on the basis of the deduced Additionally, RNA-interference (RNAi) using double-stranded RNA to knock down SK and SKR reduced the

  • Dr. GPCR and Eurofins DiscoverX Join Forces to Accelerate GPCR Drug Discovery

    GPCR , the global knowledge hub for G protein-coupled receptor (GPCR) research and education, today announced GPCR plays a critical role in educating and connecting the global GPCR community,” said Geoffrey Donsimoni GPCR’s educational programs and global GPCR community, visit https://www.ecosystem.drgpcr.com About Dr With over 180 podcast episodes , live and on-demand educational programs, and a growing partner ecosystem

  • Dr. GPCR and Celtarys Research Join Forces to Expand Access to Innovative GPCR Tools

    GPCR, the global knowledge hub for G protein-coupled receptor (GPCR) research and education, is proud GPCR’s global network, educational content, and discovery tools, visit  ecosystem.drgpcr.com . ______ With over 160 podcast episodes, live and on-demand educational programs, and a dynamic partner ecosystem

  • 📢 Early Bird Registration Ends Tomorrow! | Sep 16 - 22, 2024

    Become a Premium Member to access both courses at a reduced price. Lessons are every Thursday at 10 AM EST. 🔥 Why You Should Enroll Now: Budget-Friendly & Distinctive Educational Our goal is to ensure that education is within reach for everyone!

  • High-Content Screening for GPCR Programs: Overcoming Assay Limitations with Fluorescent Ligands

    Unlike biochemical assays, which reduce biology to a single readout, HCS captures whole-cell phenotypes Regulatory and safety constraints  that complicate workflows  • High waste-disposal requirements  • Reduced The following phases minimize batch effects, reduce imaging artifacts, and strengthen reproducibility Conclusion High-content screening continues to reshape GPCR drug discovery, offering richer biological teams working in GPCR pharmacology or cannabinoid research, these tools accelerate hit validation, reduce

  • Understanding Orthosteric Binding: The Key to Drug Action

    It can inform decisions in drug design, improving therapeutic outcomes and reducing unwanted side effects Additionally, competitive inhibitors can interfere with this binding process, leading to reduced efficacy

  • Why Mastering Pharmacokinetics Fundamentals Still Defines Discovery Success Today

    Although major advances in predictive tools have reduced PK-driven attrition, misconceptions about ADME Predictive in vitro assays have dramatically reduced this attrition—but with success comes complacency The Four Fundamental Questions of PK All pharmacokinetic strategy reduces to four deceptively simple

  • G protein-biased GPR3 signaling ameliorates amyloid pathology in a preclinical Alzheimer's disease..

    or β-arrestin signaling pathways, are leading to the development of drugs with superior efficacy and reduced , Gpr3-deficient mice display several adverse phenotypes, including elevated anxiety-like behavior, reduced contrast to Gpr3-deficient mice, G protein-biased GPR3 mice do not display elevated anxiety levels, reduced We further determined that G protein-biased signaling reduces soluble Aβ levels and leads to a decrease

  • A Note from Yamina: Building the Next Chapter of Dr. GPCR

    Capital, CRO partners, and GPCR experts to help teams move faster — from idea to discovery — while reducing platform dedicated to connecting GPCR scientists, industry experts, and innovators through research, education

  • Exclusive Access: Terry's Corner is LIVE + Your Premium Member Discount!

    GPCR Premium Members a significantly reduced access  to Terry's Corner for a limited time.  

  • Using Live-cell High-Content Screening to Characterize CB2 Ligands: Insights From 16 Synthetic Cannabinoids

    image-based data provide an additional check against off-target cytotoxicity or morphological changes, reducing Importantly, Hoechst-stained nuclei (blue) remained consistent across all concentrations, indicating that reduced tracer signal was due to receptor occupancy rather than cytotoxicity or reduced cell count. By profiling binding directly in intact HEK-293 cells, the assay reduces artefacts common in membrane-based quantitative affinity measurements with image-based validation in intact cells, the approach provides a richer

  • Dr. GPCR Spotlights Revvity’s pHSense™ Internalization Tools

    GPCR , the global nonprofit platform dedicated to advancing GPCR science through education, community GPCR  is a global nonprofit platform advancing GPCR research  through education, community, and platform

  • Optimizing HTRF Assays with Fluorescent Ligands: Time-Resolved Fluorescence in GPCR Research

    both donor (usually 620nm) and acceptor (typically 665nm) wavelengths allows for data correction , reducing introduced in HTRF between excitation and emission detection lets the background signals dissipate , reducing On top of that, smaller acceptors like d2 reduce steric hindrance, making them more efficient.

  • Exploiting Dependence of Castration-Resistant Prostate Cancer on the Arginine Vasopressin ...

    In contrast, blocking AVPR2 with a selective FDA-approved antagonist, tolvaptan, reduced cell growth. In CRPC xenografts, antagonizing AVPR2, AVPR1A, or both significantly reduced CRPC tumor growth as well endogenous ligand for arginine vasopressin receptors, and knockout of AVP in CRPC cells significantly reduced

  • Rescue of Cell Surface Expression and Signaling of Mutant Follicle-Stimulating Hormone Receptors

    Cell surface expression was severely reduced to ≤18% of wild-type (WT) for 11, modestly reduced to 66% to 84% of WT for 4, and not reduced for 2. Of the 11 with severely reduced cell surface expression, restoration to ≥57% of WT levels was achieved chaperone and can rescue cell surface expression and function of certain mutant FSHRs with severely reduced

  • Advantages of Fluorescent Probes in GPCR Assays

    temporal resolution and the need for specialized facilities including disposal, mean their use should be reduced different linker sizes and types, making it easier to find the adequate probe for a certain technique and reduce Cell fragments (such as membranes) can also be used for some assays, reducing the possibility of non-specific

  • How Fast Does a Drug Work?

    kinetic binding experiments that enable operational clarity and avoid wasted effort ✅ The ability to reduce reflects equilibrium—and when it doesn’t This is practical kinetic expertise—crafted to help drug hunters reduce

  • Biased Agonism at the GLP-1 Receptor: A Pathway to Improved Therapeutic Outcomes

    In contrast, exendin-P5, another GLP-1R agonist, is biased towards cAMP accumulation but with reduced Moreover, exendin-P5 has been observed to reduce adipose tissue size more effectively than exendin, suggesting conformation of the TM6-ECL3-TM7 axis, which is associated with their bias towards cAMP production and reduced

  • 📰 GPCR Weekly News, May 22 to 28, 2023

    Recognition and Receptor Activation in Chemokine–Chemokine Receptor Complexes Industry News Mavorixafor reduces infection rates among patients with WHIM syndrome Bristol Myers Squibb’s Investigational LPA1 Antagonist Reduces produces opioids without causing addiction or overdose – studying how this process works could help reduce

  • Effect Delta-9-tetrahydrocannabinol and cannabidiol on milk proteins and lipid levels in HC11 cells

    Our results demonstrated that THC and CBD reduced cellular viability at concentrations above 30μM and Relative to control, 10μM THC and 10μM CBD reduced mRNA levels of milk proteins (CSN2 and WAP), lipid

  • Integrating Fluorescent Ligands into Flow Cytometry: Enhancing GPCR Analysis Beyond Traditional Antibody Staining

    in the fluorophore tags, such as pH sensitive probes, can further improve signal-to-noise ratio and reduce Autofluorescence and multiplexing: Using far-red or near-infrared fluorophores can reduce background

  • Ben Clements on Rescuing Opioids with GPCR Modulators

    positive allosteric modulators (PAMs) targeting the mu-opioid receptor could preserve pain relief while reducing

  • Biotech Startup Failure: Why Teams Drift Off Course Without a Single Wrong Decision

    One more experiment to reduce risk. One more indication to keep options open. Reducing uncertainty. Preserving flexibility. Naming what is deprioritized removes silent tension and reduces unnecessary expansion. 3️⃣ Treat strategic

  • Signaling pathways activated by sea bass gonadotropin-inhibitory hormone peptides in COS-7 cells...

    expressing GnIHR were challenged with both GnIH peptides, and this stimulatory action was significantly reduced can be transduced through the PKA and PKC pathways, and GnIH can interfere with kisspeptin actions by reducing

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