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Results found for "GPCR Drug Design"
- 📰 GPCR Weekly News, July 17 to July 23, 2023
GPCR Symposium on GPCRs as Therapeutic Modalities on September 22nd. GPCR Newsletter! MPGPCR Conference (November 15 -17, 2023) Structure, Mechanism, and Drug Interactions of GPCRs, Ion Channels Specialist - Natural Sciences - Surgery Senior Scientist- Membrane Technologies Computational Protein Design GPCR Ecosystem
- Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5
November 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed treatment of psychiatric and neurodegenerative diseases, and several allosteric modulators of this GPCR libraries have complementary advantages and illustrate how access to high-resolution structures of GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE
- Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell...
Originally, β-arrestins were identified for their contribution to GPCR desensitization to agonist-mediated However, current investigations have now recognized that in addition to GPCR arresting (hence the name Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE
- Effect Delta-9-tetrahydrocannabinol and cannabidiol on milk proteins and lipid levels in HC11 cells
Read more at the source #DrGPCR #GPCR #IndustryNews
- Unlock the Hidden Lives of Receptors – Are You Ready?
Imagine you're navigating a vast terrain—not on foot, but through the shape-shifting world of GPCRs. In this exclusive Expert Drug Hunter lesson, Terry Kenakin dismantles 100 years of receptor theory and uniquely sculpt their function, and how cryptic allosteric sites are quietly reshaping the frontier of drug Step into Terry’s Vault and explore “Molecular Dynamics”—where expert drug hunters forge the future.
- 📰 GPCR Weekly News, January 16 to 22, 2023
Christopher Prior, as CEO and Reports Recent Drug Discovery Highlights Call for GPCR Papers GPCRs: Signal GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit, (February 21 - 23, 2023) Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. GPCR Jobs Postdoctoral Fellow - Molecular Dynamics Postdoc in lipid regulation of GPCRs Postdoctoral GPCR Ecosystem
- 📰 GPCR Weekly News, May 29 to June 4, 2023
Hello GPCR friends👋, Stay informed with the latest developments in GPCR research and industry news! GPCR Binders, Drugs, and more ACE2 Activation by Tripeptide IRW (Ile-Arg-Trp) Depends on the G Protein-Coupled Ions Regulating Agonist and Antagonist Binding in the Active Site of a Novel Target 5HT2BR Against Drug-Resistant GPCR Events, Meetings, and Webinars FREE Symposium - IPI Surfacing (June 15, 2023) GPCRs in drug discovery GPCR Ecosystem
- Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to inv
Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE
- 📰 GPCR Weekly News, February 27 to March 5, 2023
Industry News Design Pharmaceuticals has a new website Confo Therapeutics Announces Global Licensing Computational drug design PhD student at the Department of Drug Design and Pharmacology. Computational drug design postdoc at the Department of Drug Design and Pharmacology. Software / database development PhD student at Department of Drug Design and Pharmacology. Software / database development postdoc at the Department of Drug Design and Pharmacology.
- Lipid Modulation of a Class B GPCR: Elucidating the Modulatory Role of PI(4,5)P 2 Lipids
lipids have been shown to stabilize an active conformation of class A G-protein coupled receptors (GPCRs ) through a conserved binding site, not present in class B GPCRs. For class B GPCRs, previous molecular dynamics (MD) simulation studies have shown PI(4,5)P2 interacting conformation of GCGR through a binding site conserved across class B GPCRs but absent in class A GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- Hear the sounds: the role of G protein-coupled receptors in the cochlea
Recently, several GPCRs have been found to play important roles in the cochlea. Frizzleds and Lgrs are dominant GPCRs that regulate stem cell self-renew abilities. And A1, A2A, and CB2 activation by agonists has protective functions on noise- or drug-induced hearing Here, we review the key findings of GPCR in the cochlea and discuss the role of GPCR in the cochlea, Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter
- Dr. Simone Promel
GPCR Virtual Cafe? Join us for another virtual cafe talk to hear about the amazing work that Dr. Simone Promel / Promel Lab is doing on adhesion #GPCRs. Register here (free): https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #podcast
- Activation of the human chemokine receptor CX3CR1 regulated by cholesterol
However, the drug development of CX3CR1 is hampered partially by the lack of structural information. A much smaller conformational change of helix VI upon activation than previously solved class A GPCR-Gi Thus, our data deepen the understanding of cholesterol modulation in GPCR (G protein-coupled receptor Read more at the source #DrGPCR #GPCR #IndustryNews
- Production of human A2AAR in lipid nanodiscs for 19F-NMR and single-molecule fluorescence...
describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- 📰 GPCR Weekly News, March 27 to April 4, 2023
GPCR Binders, Drugs, and more Predicting allosteric sites using fast conformational sampling as guided Methods & Updates in GPCR Research Discovery and design of G protein-coupled receptor targeting antibodies Investigating the potential of GalR2 as a drug target for neuropathic pain. Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. GPCR Ecosystem
- Why “Displacement” Misleads You: Allosteric Binding Demystified
If your project involves GPCRs , functional selectivity , or non-traditional ligands , this session is radioligand binding but suppresses functional response, it’s not broken pharmacology—it’s biology working as designed assumptions to interpret allosteric binding data, you're likely missing critical insights—or mislabeling your drug Unlock “Allosteric Binding” Now Only in Terry’s Corner Why Terry’s Corner Drug discovery isn’t slowing Subscribe to The Kenakin Brief today ➤ #AllostericPharmacology #GPCR #BindingVsFunction #ReceptorPharmacology
- 📰 GPCR Weekly News, January 30 to February 5, 2023
GPCR Jobs Computational drug design PhD student at the Department of Drug Design and Pharmacology Computational drug design postdoc at the Department of Drug Design and Pharmacology Software / database development PhD student at Department of Drug Design and Pharmacology Software / database development postdoc at the Department of Drug Design and Pharmacology Postdoc in Bioinformatics/Data Science at Department of Drug Design and Pharmacology Scientist/Senior Scientist (Research Software Engineer) Senior Scientist
- 8th RSC / SCI symposium on GPCRs in Medicinal Chemistry. October 5-7, 2022, Verona, Italy
August 2022 "GPCRs in Medicinal Chemistry Event 8th RSC / SCI symposium on GPCRs in Medicinal Chemistry 6th September 30th September – online registration (card payments)" Read more at the source #DrGPCR #GPCR
- Exploiting Dependence of Castration-Resistant Prostate Cancer on the Arginine Vasopressin ...
We previously demonstrated that the G protein-coupled receptor (GPCR) arginine vasopressin receptor type1A AVPR1A is part of a family of GPCR's including arginine vasopressin receptor type 2 (AVPR2). Read more at the source #DrGPCR #GPCR #IndustryNews
- Functional Characterization of the Venus Flytrap Domain of the Human TAS1R2 Sweet Taste Receptor
sweet taste receptor is a heterodimeric receptor composed of two distinct G-protein-coupled receptors (GPCRs The TAS1R2 and TAS1R3 subunits are members of a small family of class C GPCRs whose members share the Read more at the source #DrGPCR #GPCR #IndustryNews
- Orthosteric vs. Allosteric Interactions: The Silent Decider of Safety and Success
For drug discovery teams navigating safety margins, biased signaling, and combination therapy design, In this lesson, you’ll learn why this distinction is not just theory, but a practical framework to design This means you can design molecules that potentiate beneficial pathways without shutting down basal signaling The result is not just cleaner assay design but a sharper decision framework for selecting, prioritizing Watch our new trailers for a preview of expert-led GPCR training designed for scientists and drug hunters
- Structure of the vasopressin hormone-V2 receptor-β-arrestin1 ternary complex
October 2022 "Arrestins interact with G protein-coupled receptors (GPCRs) to stop G protein activation Recent structural studies shed light on the molecular mechanisms involved in GPCR-arrestin coupling, but whether this process is conserved among GPCRs is poorly understood. It reveals an atypical position of β-arrestin1 compared to previously described GPCR-arrestin assemblies Read more at the source #DrGPCR #GPCR #IndustryNews
- Arginine 125 Is an Essential Residue for the Function of MRAP2
helps in elucidating the metabolic pathways involved in metabolic dysfunction and in developing new drugs Read more at the source #DrGPCR #GPCR #IndustryNews
- Adenosine receptor signalling in Alzheimer's disease
Emerging evidence suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets into some novel strategies, including allosterism and the targeting of oligomers, which may increase drug Read more at the source #DrGPCR #GPCR #IndustryNews
- Regulators of G-protein signaling: essential players in GPCR signaling
components of the intracellular signaling pathways that mediate the effects of G protein-coupled receptors (GPCRs Upon activation, GPCRs have conformational changes that allow the coupling and subsequent activation Role of RGS proteins in regulating GPCR signaling: Recent studies have revealed that the interaction The interaction between RGS proteins and GPCRs is highly specific and tightly regulated; mutations in and amplitude of GPCR signaling.
- Adenosine receptor signalling in Alzheimer's disease
Emerging evidence suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets into some novel strategies, including allosterism and the targeting of oligomers, which may increase drug Read more at the source #DrGPCR #GPCR #IndustryNews
- Targeting mGluR2/3 for treatment of neurodegenerative and neuropsychiatric diseases
Therefore, mGluR2 and mGluR3 have been considered as potential drug targets for the treatment of many Alzheimer's disease, Huntington's disease, Parkinson's diseases, schizophrenia and depression as well as drug We then highlight the evidence supporting the use of various drugs including orthosteric and allosteric Read more at the source #DrGPCR #GPCR #IndustryNews
- Diversification of PAR signaling through receptor crosstalk
Read more at the source #DrGPCR #GPCR #IndustryNews
- New structural perspectives in G protein-coupled receptor-mediated Src family kinase activation
Sandra Berndt talk about new structural perspectives in GPCR-mediated Src family kinase activation. Register here (FREE) https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe #drgpcr #gpcr #virtualcafe
- GRK2 in cardiovascular disease and its potential as a therapeutic target
G protein-coupled receptors (GPCRs) are critical myocardial signal transducers which regulate cardiac Additionally, GPCR dysregulation underlies multiple models of cardiac pathology, and most pharmacological A recent focus on GPCR intracellular-regulating proteins such as GPCR kinases (GRKs) has uncovered GRK2 These data support the premise that GRK2 should be at the forefront of a novel investigative drug search Read more at the source #DrGPCR #GPCR #IndustryNews





