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Results found for "preclinical pharmacology"

  • Pharmacologic Models

    Are you ready to truly understand how pharmacologists predict whole-body drug response from a single straight to it:   Why models are vital for translating lab data into clinical forecasts The 4 types of pharmacologic Elevate your pharmacology expertise. Unlock "Pharmacologic Models" now

  • Pharmacology at Your Fingertips: Terry’s Corner Launches

    Welcome Back, Discovery Drivers   Terry’s Corner is live, on-demand pharmacology built for drug discovery Dr.GPCR Updates Terry’s Corner is Live - Pharmacology at your fingertips Terry’s Corner is now open! and scalable systems, it turns scattered data into decisions, accelerating your path to a successful preclinical Better pharmacology leads to better decisions—unlock it now with Terry’s Corner.

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

    reduces soluble Aβ levels and leads to a decrease in the area and compaction of amyloid plaques in the preclinical provide proof of concept for the development of safer GPCR-targeting therapeutics with more directed pharmacological

  • Misread the Curve, Misjudge the Drug: Rethinking Antagonism in GPCR Pharmacology

    When pharmacologists misinterpret how an antagonist interacts with its receptor, the consequences ripple Terry Kenakin reframes one of pharmacology’s most foundational ideas: the difference between competitive Inside the Lesson: Antagonist Behavior by the Numbers Terry walks through both the pharmacologic and If you want to avoid costly misinterpretations and strengthen your pharmacology toolkit, Terry’s Corner Brief today  ➤   #GPCRantagonism #CompetitiveAntagonists #NonCompetitiveAntagonists #DoseResponseCurve #Pharmacology

  • Why Dose-Response Curves Are Pharmacology’s Secret Weapon

    In the newest foundational lesson from Terry Kenakin’s Pharmacology Vault , we unlock the visual language of pharmacology: dose-response curves . 👉 Discover why dose-response curves are the backbone of all pharmacology.

  • Accelerating GPCR Drug Discovery: What 40 Years of Pharmacology Reveal

    Attrition rates in early pharmacology remain painfully high. The High Cost of Pharmacology Gaps Every experienced drug hunter knows this: validation isn’t the problem Terry puts it bluntly: “Once you have a molecule, everything boils down to pharmacology—hit, lead, candidate invaluable for mechanistic understanding—assay volume control, expression system contrasts, predictive pharmacology Corner Terry’s Corner  is a living, growing knowledge hub led by Terry Kenakin—a world authority in pharmacology

  • Enzyme Inhibition Pharmacology: The Hidden Gatekeepers of GPCR Drug Discovery

    Recognizing, predicting, and leveraging these interactions is the essence of enzyme inhibition pharmacology This lesson reframes enzyme interaction not as background noise, but as a core pharmacological event. Clark , laid the foundation for today’s quantitative pharmacology. Enzyme Inhibition Pharmacology: Orthosteric vs. Pharmacology isn’t just about hitting the receptor—it’s about surviving the enzymes first.

  • Pharmacology Isn't What You Think—It's So Much More

    Welcome to Terry’s Corner , where foundational pharmacology is demystified by someone who’s spent over In his newest lesson, “The Uniqueness of Pharmacology in Drug Discovery,” Terry Kenakin explains why pharmacology isn’t a clean-cut science—it’s a dynamic dialogue between molecule and system. You’ll uncover: Why pharmacology is the glue between chemistry and biology How to interpret drug behavior the story it’s telling. 👉 Start your journey with Terry’s foundational series Unlock "Unique Role of Pharmacology

  • Competitive vs Non-Competitive GPCR Antagonists: How to Interpret Pharmacology Data with Confidence

    Welcome back GPCR lovers, In pharmacology, the wrong interpretation of antagonist behavior can derail This week in Terry’s Corner , we go beyond the dose-response curves to explore the kinetic and pharmacologic edge by staying on top of the latest breakthroughs in allostery, biased signaling, and computational pharmacology Keywords: GPCR, drug discovery, pharmacology, antagonism, competitive, non-competitive, Terry's Corner excellence, drug development, pharmaceutical, scientific career Hashtags: #DrGPCR #GPCR #DrugDiscovery #Pharmacology

  • Why “Displacement” Misleads You: Allosteric Binding Demystified

    using the Hall allosteric cube The Allosteric Shift: When Receptors Become Something New In orthosteric pharmacology Function: Two Different Worlds One of the most common—and dangerous—mistakes in allosteric pharmacology When a PAM increases radioligand binding but suppresses functional response, it’s not broken pharmacology—it The takeaway:  what looks like pharmacology failure may be a systems problem . Terry Kenakin An always-growing library of on-demand pharmacology insights The ability to vote on or

  • Are You Guessing or Forecasting? Master GPCR Pharmacologic Models Before It’s Too Late

    Terry's Corner - New Course on Pharmacologic Models The latest Terry’s Corner unlocks clinical forecasting in the full newsletter   Secure Your Access Now ➤ 🗣️ “Thank you for bringing this (Principles of Pharmacology

  • From Ox Liver to AI: How the History of Pharmacology Shapes Its Future

    Terry Kenakin takes you on a captivating tour through the history of pharmacology : a journey that spans Whether you're stepping into pharmacology for the first time or rekindling your interest, this lesson Terry’s Corner, your essential launchpad into the world of therapeutic science Unlock "The History of Pharmacology

  • Job Opportunity Spotlight #1: Principal Scientist, In Vitro Pharmacology

    As Chief Matchmaker, I recently had the pleasure of speaking with Beth Fleck, Director of In Vitro Pharmacology Beth is also the hiring manager for their open Principal Scientist, In Vitro Pharmacology role posted Top candidates will have a solid foundation in GPCR pharmacology as well as some experience in drug discovery

  • Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment of...

    October 2022 Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment The network pharmacology method was used to constructe the "herb-component-target" network, and elucidated

  • How GPCR Spatial Signaling Sparked a Scientific Journey

    From Cambridge to Leadership That early curiosity led her to pursue a PhD in Molecular Pharmacology at Summer Project  — Unexpected spark PhD at Monash  — From curiosity to expertise Cambridge Fellowship  — Precision is organized in time and space, her team is opening doors to next-generation GPCR drug discovery and precision

  • Exploring pharmacological inhibition of G q/11 as an analgesic strategy

    The aim of this study was to test this hypothesis pharmacologically by using potent and selective Gq/

  • Pharmacological Properties and Function of PxOctβ3 Octopamine Receptor in Plutella xylostella (L.)

    This study demonstrated the pharmacological properties and functions of PxOctβ3 in P. xylostella, thus

  • A robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.

    Cannabinoids as Anticancer Drugs: Current Status of Preclinical Research. Acta Pharmacol Sin   2019 , 40  (3), 324–335. https://doi.org/10.1038/s41401-018-0164-x . (8)         J Pharmacol Exp Ther   1996 , 278 (3), 989–999. (12)      Martín-Fontecha, M.; Angelina, A.; Rückert Pharmacological Evaluation of New Constituents of “Spice”: Synthetic Cannabinoids Based on Indole, Indazole 1,4-Dihydroquinoline-3-Carboxamide Derivatives as New CB2 Cannabinoid Receptors Agonists: Synthesis, Pharmacological

  • Dynamics of tumor-associated macrophages in a quantitative systems pharmacology model of...

    September 2022 Dynamics of tumor-associated macrophages in a quantitative systems pharmacology model of immunotherapy in triple-negative breast cancer "Quantitative systems pharmacology (QSP) modeling is

  • Terry’s Corner, Celtarys' Leap, and the $7B GPCR Horizon

    Hello GPCR Minds,   This week, you'll learn all about Terry’s Pharmacology Corner, your new learning space focused on GPCR pharmacology. GPCR Updates Learn Pharmacology That Drives Discovery  – From Dr. Terry Kenakin   Terry’s Corner is your space focused on GPCR pharmacology designed just for you.  

  • Understanding Enzyme Inhibition In GPCR Discovery Programs

    Breakthroughs this week:  Potentiation of GPCR signaling by ATP and sugar monophosphates; Pharmacology You’ll explore how catalytic control, allosteric shifts, and CYP450 behavior rewrite the rules of pharmacology Kenakin — October 30, 12 PM EST Bring your toughest pharmacology questions and join Dr. GPCR scientists, translational pharmacologists, biotech discovery teams, and decision-makers who need

  • How Fast Does a Drug Work?

    How do competing ligands slow or alter binding rates, and what does this tell you about real-world pharmacology candidates faster Unlock “Drug Binding Kinetics” Now Only in Terry’s Corner   ______ #DrugDiscovery #Pharmacology

  • Differential binding of Δ9-tetrahydrocannabinol derivatives to type 1 cannabinoid receptors (CB1)

    This interest has been driving efforts to understand their pharmacology since the 1980s. CELT-335 was successfully used in assays to determine the pharmacological properties of Δ9-tetrahydrocannabinol binding of naturally occurring Δ9-tetrahydrocannabinolderivatives to cannabinoid CB1 and CB2 receptors, Pharmacological Zagzoog A et al ., In vitro and in vivo pharmacological activity of minor cannabinoids isolated from Tetrahydrocannabinolic acid alleviates collagen-induced arthritis: Role of PPARγ and CB1 receptors, British Journal of Pharmacology

  • Radioligands vs. Fluorescent Ligands: Binding Assays

    field, assays have shifted towards fluorescent-approaches, thanks to their versatility, safety and precision optimization ensure access to the binding site with minimal unspecific interactions, while also tuning the pharmacological accessible alternative. -            Quantitative cell binding studies : Radioligands have superior precision Br J Pharmacol. 2020 Mar;177(5):978-991. doi: 10.1111/bph.14953. Probing the pharmacology of G protein-coupled receptors with fluorescent ligands.

  • Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and...

    October 2022 Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and Pharmacological targeting of cGAS/STING-YAP signaling by both a small-molecule STING agonist, SR-717, Further, pharmacological targeting of cGAS/STING-YAP axis exhibits the potential to alleviate liver and

  • Applying Allosteric Modulator Pharmacology to Treat Dyskinesia and Other Movement Disorders with ...

    April 2022 Applying Allosteric Modulator Pharmacology to Treat Dyskinesia and Other Movement Disorders Addex Therapeutics "Tim Dyer is the Co-Founder and CEO of Addex Therapeutics, which is focusing on the pharmacology

  • 📰 GPCR Weekly Buzz: Exciting Schedule Shifts for Principles of Pharmacology I & II | August 12-18, 2024

    We’ve made some updates to the Principles of Pharmacology I & II courses, and we can’t wait for you Here’s the refreshed schedule: Principles of Pharmacology I October 3, 10, 17, 24 Principles of Pharmacology Don’t miss out on insightful resources like '   Applying Pharmacology to Drug Discovery ' and ' Advanced Data Analysis for GPCR Pharmacology .' Don’t miss your chance to dive into the Principles of Pharmacology I & II BUNDLE .

  • Predicting GPCR Function: Inside the Carlsson Lab’s Modeling Toolbox

    For decades, GPCRs have been the cornerstone of pharmacology. Projects in his group often begin with either: A new GPCR structure  ripe for exploration, or A pharmacological Carlsson’s group integrates modeling with mechanistic pharmacology. improved GPCR structures, and scalable experimental assays is shrinking the gap between modeling and pharmacology Forward The Carlsson lab exemplifies how c omputational biochemistry can meaningfully impact real-world pharmacology

  • Why Kinetics Matter More Than Kd in GPCR Drug Discovery

    Career opportunities:  Principal Scientist - In Vitro Pharmacology; Senior Scientist, Molecular Pharmacology Weekly News : jobs, events, papers, industry updates Exclusive discounts on Terry’s Corner  digital pharmacology access to insights from major conferences, emerging research, and expert commentary Whether you’re a pharmacologist GPCR scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who Edition here ➤    Access all the news and upcoming events Hashtags: #GPCR #DrGPCR #BindingAffinity #Pharmacology

  • Fluorescence based HTS compatible ligand binding assays for dopamine D3 receptors in baculovirus preparations and live cells

    Pharmacology & Therapeutics   2016 , 165 , 164–177. https://doi.org/10.1016/j.pharmthera.2016.06.007 European Journal of Pharmacology   2017 , 799 , 58–66. https://doi.org/10.1016/j.ejphar.2017.01.040 . European Journal of Pharmacology   2018 , 839 , 40–46. https://doi.org/10.1016/j.ejphar.2018.09.008 . Trends in Pharmacological Sciences   2018 , 39  (2), 187–199. https://doi.org/10.1016/j.tips.2017.10.004 Biochemical Pharmacology   1973 , 22 (23), 3099–3108. https://doi.org/10.1016/0006-2952(73)90196-2 .

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