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- 📰 GPCR Weekly News, June 26 to July 2, 2023
Function Identification of a potential structure-based GPCR drug for interstitial cystitis/bladder pain syndrome
- ⛵Sailing the GPCR Seas: Your Weekly Research Voyage! ⦿ Nov 11 - 17, 2024
announces the positive results of its clinical Phase 1/2 Study with AEF0217 in young adults with Down syndrome
- 📰 GPCR Weekly News
Identification of a potential structure-based GPCR drug for interstitial cystitis/bladder pain syndrome
- Fluorescence based HTS compatible ligand binding assays for dopamine D3 receptors in baculovirus preparations and live cells
Guidelines for the First-Line Treatment of Restless Legs Syndrome/Willis–Ekbom Disease, Prevention and
- Reflections on My PhD Journey: Lessons Learned
The Importance of Experimental Controls Experiments are at the heart of a PhD in the sciences, and one key lesson I’ve learned is the importance of rigorous controls. and goals, embrace the discipline of structured research and analysis, and never underestimate the importance
- High-Content Screening for GPCR Programs: Overcoming Assay Limitations with Fluorescent Ligands
However, their limitations become increasingly important as drug discovery moves toward high-information Retaining single-cell data preserves heterogeneity and enables mechanistic analyses, particularly important readout clarity, strengthens data reproducibility, and enables kinetic or equilibrium measurements impossible
- Unlock the Hidden Complexity Behind GPCRs—From Terry Kenakin’s Vault
What if the way we've been studying GPCRs—arguably the most important drug targets in pharmacology—has
- Advancements in G protein-coupled receptor biosensors to study GPCR-G protein coupling
Their applications have continually expanded our understanding of this important protein class. Here, we briefly summarize a subset of this field with accelerating importance: transducer biosensors
- Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology, behavior...
: Insight from pharmacology, biology, behavior, and neurophysiology "The awareness of the potential importance We now summarize important pharmacological, molecular, and cellular studies relevant to D1-mediated β-arrestin-related We discuss the importance of understanding the translatability of cell and animal models to have more
- Ever Wondered How Drugs Are Discovered?
essential Why target-based discovery is powerful, but can miss the forest for the trees The critical importance
- Maria’s Travel Blogs: ACSMEDI-EFMC Medicinal Chemistry Frontiers 2025
Sometimes when you’re in the field you forget the importance GPCRs holds in drug development as a whole Another section was dedicated to Chemistry Tools, highlighting their importance.
- Understanding the Journey: Catherine Demery's Path to Addiction Science
The Importance of Passion in Research Catherine's journey highlights the importance of passion in research Her journey illustrates the power of following one's passion and the importance of being adaptable in
- G protein-coupled receptor signaling: transducers and effectors
October 2022 "G protein-coupled receptors (GPCRs) are of considerable interest due to their importance pathways, dynamic structures, and physiological relevance in the cardiovascular system of the three most important
- Beyond the Probe: Scaling Innovation From the Bench to Product Launch
Maria emphasizes the importance of genuinely listening to researchers: understanding the biological question
- AlphaFold2 versus experimental structures: evaluation on G protein-coupled receptors
August 2022 "As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide Recently, AlphaFold2 has been developed to predict structure models of many functionally important proteins
- 📰 GPCR Weekly News, April 29 to May 5, 2024
We also have some important announcements in today’s episode, so join us in this celebration and be the
- Modulation of Striatal Adenosinergic Function by HTL0041178, a Selective GPR52 Agonist
Cliona MacSweeney, a project director in our Translational Medicine department, recently presented this important This work highlights an important interplay between the adenosinergic and dopaminergic systems and suggests
- Transmembrane domains of GPCR dimers – a novel hot spot for drug discovery
In this study Xin Cai et al. highlight the importance of GPCR dimers in drug discovery referring to important An important example of a GPCR forming both monomers and dimers with distinct functions in respect to be activated and interact with G proteins and therefore preserve their physiological functions, an important
- Combined docking and machine learning identify key molecular determinants of ligand pharmacological
structures that mediate their action and that among a large dataset of different ligands, the functionally important antagonist ligands made interactions with W2866.48×48 and Y3167.43×42, both residues considered to be important
- GPCR Pharmacology Insights That Prevent Real Drug Discovery Failures
Allosteric Modulators: System-Conscious Control Orthosteric ligands displace native signaling and impose Receptor Density: The Distortion Engine One of the AMA’s recurring themes was the impossibility of interpreting
- Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs)...
tissue compared with adjacent normal tissue of HCC patients; (b) RGS20 was strongly associated with some important alpha-fetoprotein and tumor grade in the HCC patients; (c) besides HCC (p < 0.001), RGS20 was found to be an important
- GPCR/endocytosis/ERK signaling/S2R is involved in the regulation of the internalization...
have shown that fluorescently labeled Hst1 (F-Hst1) targets and activates mitochondria, presenting an important showed the intracellular trafficking and targeting process of F-Hst1, in which early endosome plays an important
- Ginsenoside Rg5 allosterically interacts with P2RY12 and ameliorates deep venous thrombosis by...
DVT formation is a time-dependent inflammatory process in which NETosis plays an important role.
- The Five Traps of Ignoring Kinetics
You calculate an equilibrium value that requires a physically impossible onset rate. This is the second trap: trusting impossible math. If you ignore it, you risk false certainty.
- Mechanistic basis of GPCR activation explored by ensemble refinement of crystallographic structures
October 2022 "G protein-coupled receptors (GPCRs) are important drug targets characterized by a canonical
- Targeted Drug Design through GPCR Mutagenesis: Insights from β2AR
This case study underscores the critical importance of mutagenesis in GPCR research. Interestingly, only 10 out of 82 important residues are within the ligand-binding pocket, resulting in
- Specific Functions of Melanocortin 3 Receptor (MC3R)
In this review paper, we aimed to point out the importance of the MC3R regulations in three main concepts
- Diversification of PAR signaling through receptor crosstalk
beginning to be explored and represents a novel mechanism providing diversity to receptor function and play important
- The mouse cytomegalovirus G protein-coupled receptor homolog, M33, coordinates key features of ...
IMPORTANCE G protein-coupled receptors (GPCRs) act as cell surface molecular "switches" which regulate date possess GPCR homologs with phylogenetic evidence for independent gene capture events, signifying important The mouse CMV (MCMV) GPCR homolog, designated M33, is important for cell-associated virus spread and
- Structural view of G protein-coupled receptor signaling in the retinal rod outer segment
(GPCR) signaling pathway because of its quantifiable stimulus, non-redundancy of genes, and immense importance











