Search Results

G protein-coupled receptors (GPCRs) are among the most promising drug targets. Specifically controlling the activity of GPCR dimers with ligands is a good approach to clarify their The data support the inference that they act at the active interface between both transmembrane domains Overall, these data reveal the possibility of developing allosteric compounds able to specifically modulate the activity of GPCR homo- and heterodimers by acting at their transmembrane interface.

Read more at the source #DrGPCR #GPCR #IndustryNews

Therefore, the newest data related to TRPM3 have to be discussed and to be put in context as soon as possible to be up-to-date and to accelerate the translation from bench to bedside. Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

localization, potentially scaffolding distinct signaling platforms. Emerging strategies incorporate unnatural amino acids and crosslinking for structural data inference GPCR–β-Arrestin complexes: versatile scaffolding platforms β-arrestins exhibit interactions with over By comparing β-arrestin expression data in healthy tissues from the Genotype-Tissue Expression (GTEx) database with data from cancer samples in The Cancer Genome Atlas (TCGA) through the Gene Expression

Imagine running a calcium assay and discovering your compound shows only weak activity. What if that result wasn’t telling you the whole story? In this foundational lesson, Terry Kenakin dives deep into a widely used, often misunderstood tool in early drug discovery: the calcium assay. Revered for its convenience, the FLIPR assay provides rapid insights into receptor activity. But its speed comes with a cost. You’ll learn why calcium signals are inherently transient—giving rise to a “hemi-equilibrium” window that can significantly distort your understanding of drug potency. Through real-world examples (like 5-HT2A and CCR5 agonists), Terry shows how slow-onset agonists can be drastically underestimated—potentially leading promising leads to be dismissed too early. Why does this matter? Because when true pharmacological profiling is essential—like detecting partial or inverse agonism—calcium assays just don’t deliver. If you're starting out in pharmacology, this lesson gives you the interpretive tools to ask smarter questions, avoid missteps, and use calcium assays with strategic clarity. 📍 Foundational Level | Calcium Assays 📚 Part of Terry Kenakin’s Pharmacology Vault 👉 Curious what else you've been missing? Unlock "Calcium Assays" now

G protein-coupled receptors (GPCRs) have been shown to play integral roles in Alzheimer's disease pathogenesis However, it is unclear how diverse GPCRs similarly affect Aβ and tau pathogenesis. GPCRs share a common mechanism of action via the β-arrestin scaffolding signaling complexes, which not only serve to desensitize GPCRs by internalization, but also mediate multiple downstream signaling events As signaling via the GPCRs, β2-adrenergic receptor (β2AR), and metabotropic glutamate receptor 2 (mGluR2

Molecular innovation This Week’s GPCR Intelligence: The next edge in discovery isn’t louder exposure—it Breakthroughs this week:  nanomedicines targeting PAR2 for sustained analgesia; Emerging Voices in GPCR GPCR Premium: Sneak Peek Industry insights:  Confo VLAIO grant; Skye CB1 Ph2 miss; Chugai CT-388 in-license Upcoming events:  Membrane-mimetic screening; GPCR Forum 2025; GPCR-TDD Summit Europe. GPCR scientists, translational pharmacologists, biotech discovery teams, and decision-makers who need

You don’t need more data—you need a way to translate snapshots into predictions. Garbage In, Garbage Out Even the best models can only work with the data they’re fed. The lesson: models don’t just need data. They need the right data . Only when the data were fit to the right model did the picture snap into focus. The pace of GPCR innovation is accelerating—teams acting on today’s insights will set tomorrow’s standards

What is the molecular basis that determines that GPCRs bind selectively or promiscuously to different The discovery of the orthosteric binding pocket is of great importance in GPCRs field as it supports Additionally, structural analysis of the TM5 and TM6 regions of 27 class A GPCRs coupled to Gs or Gi/ 2.6 ± 1.6 residues shorter, concluding that the TM5-TM6 macro-switch length is conserved in class A GPCRs #GPCR #DrGPCR

GPCR podcast! 🥁 Drum rolls, please! Our guest is the wonderful Dr. Rosie Dawaliby! GPCR Ecosystem paid membership ➡️ https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ep-84-with-rosie-dawaliby #gpcr #drgpcr

GPCR Summit from October 10th to the 16th is taking shape. GPCR Ecosystem site member, which is free! Sign up now ➡️ https://bit.ly/3eaO5PH #gpcr #drgpcr

GPCR Summit 2022. This is a great opportunity for us to come together and talk GPCRs. Join us now ➡️ https://www.ecosystem.drgpcr.com/dr-gpcr-summit-2022 #gpcr #drgpcr

demonstrate that the chemoreceptor genes, srg-36 and srg-37, which encode G protein-coupled receptors (GPCRs Here, we show that SRG-36 and SRG-37 act as upstream GPCRs that activate EGL-30. SRG-36 and SRG-37 are GPCRs for the dauer-inducing ascaroside, ascr#5. Thus, ascaroside signaling promotes axon regeneration by activating the GPCR-Gqα pathway.

GPCR Summit 2022. Mark your calendar for October 10th and 16th. ➡️ https://www.ecosystem.drgpcr.com/ #gpcr #drgpcr

Chemokine receptors (CKRs) belong to a subfamily of G-protein-coupled receptors (GPCRs) and play a crucial Currently, there are more than 40 available structures of chemokines and their receptors in the Protein Data helix (TM7) near ECL3, while the other links TM3 with ECL2, which is common to the broader class A GPCR In addition, it has a glutamate residue at position 3.45, which is not found in human class A GPCRs, Check the original article at https://pubmed.ncbi.nlm.nih.gov/37212620/ #GPCR #DrGPCR #Ecosystem

➡️ https://bit.ly/3wQNZDg #gpcr #drgpcr

β-arrestins (βarrs) play multifaceted roles in the function of G protein-coupled receptors (GPCRs). βarrs typically interact with phosphorylated C-terminal tail (C tail) and transmembrane core (TM core) of GPCRs changes for βarr activation upon the C tail- and TM core-mediated interactions with a prototypical GPCR This plasticity of βarr conformation in complex with GPCRs engaged in different binding modes may explain

and precision-engineer therapeutics with enhanced potency and tailored signaling against an undrugged GPCR #ai #drugdiscovery #gpcr" Read more at the source #DrGPCR #GPCR #IndustryNews

describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR Protocols for SMF experiments include sample setup, data acquisition, data processing, and error analysis Read more at the source #DrGPCR #GPCR #IndustryNews

ubiquitously expressed membrane proteins that associate with different G protein–coupled receptors (GPCRs ), including the parathyroid hormone 1 receptor (PTH1R), a class B GPCR and an important modulator of These data uncover a critical role of RAMPs in the activation and signaling of a GPCR that may provide a new venue for highly specific modulation of GPCR function and advanced drug design." Read more at the source #DrGPCR #GPCR #IndustryNews

November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially Although GPCRs are primarily found at the plasma membrane, GPCRs can traffic to and signal from many subcellular signaling contributes to the biased signaling generated by three endogenous ligands of the GPCR observed at CXCR3, which has important implications for drugs targeting chemokine receptors and other GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE

The C5aR1 is a classical G-protein-coupled receptor (GPCR), whereas C5aR2 is a nonclassical GPCR that The computational modeling and the 1.5-μs molecular dynamics data presented in the current study are Read more at the source #DrGPCR #GPCR #IndustryNews

STING-YAP signaling by both a small-molecule STING agonist, SR-717, and a G protein-coupled receptor (GPCR Together, our data support that activation of cGAS/STING signaling mitigates organ fibrosis and suppresses Read more at the source #DrGPCR #GPCR #IndustryNews

GPR15 is a G protein-coupled receptor (GPCR) located on chromosome 3 and has similarity in its sequence The expression of GPR15 and c10orf99/gpr15l mRNA was analyzed by RT-qPCR. Statistical analysis included Kruskal-Wallis test, T-test, or Mann-Whitney U test, according to data Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "G protein-coupled receptors (GPCRs) are of considerable interest due to their importance dynamic structures, and physiological relevance in the cardiovascular system of the three most important GPCR signaling effectors: heterotrimeric G proteins, GPCR kinases (GRKs), and β-arrestins. As new technologies are developed and applied to studying GPCR structure and their downstream effectors Read more at the source #DrGPCR #GPCR #IndustryNews

In this review, we focus on recent advances in G-protein-coupled receptor (GPCR) targets. To date, the most promising targets are the chemokine, cannabinoid, and dopamine receptors, but future

therapeutic targets in Uterine Corpus Endometrial cancer "Adhesion G protein-coupled receptors (adhesion GPCRs ), as a member of the G protein-coupled receptors (GPCRs) superfamily, have gradually entered the field The structure, function, and involvement of adhesion GPCRs in cancer development have been discussed alsooneofthemostcommonfemalereproductivesystemtumors, but there are few pieces of research related to adhesion GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews

Data on platelet activation are extrapolated across experimental settings. Read more at the source #DrGPCR #GPCR #IndustryNews