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- C5aR2 receptor: The genomic twin of the flamboyant C5aR1
Currently, the exact function of the C5aR2 is actively debated in the context of C5aR1, even though both
- Adrenal G Protein-Coupled Receptors and the Failing Heart: A Long-distance, Yet Intimate Affair
Chronic human HF is characterized by several important neurohormonal perturbations, emanating from both
- Target Residence Time: The Hidden Driver of In Vivo Efficacy
therapeutic window ✅ Examples of how rebinding in dense receptor environments amplifies target occupancy, even
- How Fast Does a Drug Work?
a ligand binds (k₁) and how long it stays bound (k₂) can alter therapeutic profiles dramatically, even
- Conjugation Strategies for Probe Development
NHS esters are not very stable even in aqueous environment but they only need a slightly basic medium
- GPCR Allosteric Modulation: Why Allostery is the Engine of Drug Discovery
Ligands may take hours to equilibrate , even when they look potent on paper.
- Is Your GPCR Drug Discovery Program Built for Breakthroughs or Breakdowns?
your science isn't continuously integrated with your GPCR operational strategy and investment goals, even
- Enhancing GPCR Research Outreach | Dr GPCR University early-bird registration ends soon!
We've got 11 GPCR papers, seven industry news pieces, a new GPCR event, and even a job ad.
- Unveiling GPCR Priming: The Hidden Synergy in Cellular Signalling
Surprisingly, this interaction did not result in G12 activation, even in the presence of GTP, which is
- Your GPCR Program Decisions Depend on Good Data Interpretation
But Terry Kenakin’s new Emerging Drug Hunter lecture reveals why this assumption can mislead even experienced
- Extracellular signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery
The gravity of this regulation becomes even more apparent when we consider the potential consequences
- Therapeutic validation of an orphan G protein‐coupled receptor
Some studies have also reported GPR84 involvement in pain, atherosclerosis, and even metabolic disorders
- Advantages of Fluorescent Probes in GPCR Assays
At Celtarys, we focus on developing fluorescent tools that keep minimal background signal even without
- Competitive vs Non-Competitive GPCR Antagonists: How to Interpret Pharmacology Data with Confidence
the wrong interpretation of antagonist behavior can derail your conclusions, your experiments, and even
- 📰 GPCR Weekly News, May 13 to 19, 2024
And here's something even better: the video versions of our podcast episodes are now available to the
- GPCRs are not simple on-off switches: deep dive into GPCR-ligand interactions
absence of G proteins (Gether 2000), with numerous intermediate sub-states in between (Vauquelin and Van and can differ in intrinsic efficacy; 2) partial agonists are incapable of inducing maximal activity even
- Glyco-sulfo hotspots in the chemokine receptor system
In addition, tyrosine sulfation is heterogenous between cell lines or even on the same cell (Scurci I
- Artificial intelligence – faster, smarter, cheaper GPCR drug discovery
Baek et al., 2021) allow the prediction of the 3D structure of a protein from the amino acid sequence even
- Structural landscape of the Chemokine Receptor system
US28 evolved high constitutive activity to evade host immunity, whereas ACKR3 functions as a homeostatic
- A robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.
validation, a larger range of compounds will be tested, including screening chemical libraries with even 999. (12) Martín-Fontecha, M.; Angelina, A.; Rückert, B.; Rueda-Zubiaurre, A.; Martín-Cruz, L.; Van , S.; Beck, J.; Nettekoven, M.; Benito-Cuesta, I.; Grande, T.; Drawnel, F.; Widmer, G.; Holzer, D.; Van V.; Van Der Stelt, M.; Pacher, P.; Gertsch, J.; Ullmer, C.; McCormick, P. J.; Oddi, S.; Spaink, H.