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- 📰 GPCR Weekly News, January 30 to February 5, 2023
For Dr. GPCR News, please subscribe to your monthly newsletter. Research Fellow - School of Physics and Astronomy Postdoctoral Research Associate (Fixed Term) Explore Dr
- Why “Displacement” Misleads You: Allosteric Binding Demystified
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- 📢 GPCR Update: August 19-25, 2024 | Thrilling Announcement: New Pharmacology Course Dates & Exclusive Discounts Inside!
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- GPCR Allosteric Modulation: Why Allostery is the Engine of Drug Discovery
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- Why Intracellular Drugs May Hold the Key to GPCR Therapeutics
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- How GPCR Collaboration Built an Innovation Engine
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- 📰 GPCR Weekly News - January 2 to 8, 2023
Receptor 2 In Diabetic Retinopathy PhD Opportunity - Novel P2y Receptor Ligands For Drug Discovery Explore Dr
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- How Collaboration Drives GPCR Discoveries
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- 📰 GPCR Weekly News, January 23 to 29, 2023
of Staff Postdoctoral Fellow, Biochemical And Cellular Pharmacology Project Leader, Biology Explore Dr
- 📰 GPCR Weekly News - January 9 to 15, 2023
Receptor 2 In Diabetic Retinopathy PhD Opportunity - Novel P2y Receptor Ligands For Drug Discovery Explore Dr
- Accelerating GPCR Drug Discovery: What 40 Years of Pharmacology Reveal
Monthly AMAs where you can challenge Dr. Kenakin with your own enzyme or GPCR interaction puzzles.
- 📰 GPCR Weekly Buzz: Exciting Schedule Shifts for Principles of Pharmacology I & II | August 12-18, 2024
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- GPCR Buzz of the Week | Sep 23 - 29, 2024
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- Adhesion GPCR Consortium Newsletter - May 2024
postdoctoral training, I joined one of the labs that participated in Latrophilins’ discovery, the lab of Dr
- From Student to Mentor: What Alessandro Nicoli Learned About Leading in Science
Antonella Di Pizio’s lab , there was almost nothing—no team, no culture, not even proper desks. Over the years you see the lab establishing, and for both of us, of course, growing.”
- A robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.
New scaffolds modulating the CBRs in both the orthosteric and allosteric sites have been developed, supported Their binding affinity was assessed through radioligand binding, showing a nanomolar affinity for both , both agonists and antagonists. Indeed, the difference is lower than 1pKi value between both experiments. L.; Miljuš, T.; Mexi, M.; Roth, N.; Koers, E. J.; Guba, W.; Alker, A.; Rufer, A. C.; Kusznir, E.
- High-Content Screening for GPCR Programs: Overcoming Assay Limitations with Fluorescent Ligands
When executed as a unified pipeline, these phases ensure an HCS assay capable of supporting both exploratory Their ability to visualize ligand–receptor interactions directly in living cells produces data that are both Visual + Quantitative Data Fluorescent ligand assays generate both numerical values (IC₅₀, Kᵢ) and spatial Lin S, Schorpp K, Rothenaigner I, Hadian K. Image-based high-content screening in drug discovery.
- Applications of Fluorescent Probes in Confocal Imaging of GPCRs: From Live to Fixed Cells
Studying their dynamics in both a spatial and temporal manner is key to understanding how they work in fluorescent probes must have high specificity, minimal phototoxicity and preferably be compatible with both This is why fluorescent tags, both attached to the protein or to pharmacophores, are so interesting. image stacks, facilitating the reconstruction of GPCR distribution in tissue-like environment , in both
- Class B1 GPCR Dimerization: Unveiling Its Role in Receptor Function and Signaling
C GPCRs, are obligate dimers, either as homodimers or heterodimers, with distinct conformations in both Recent studies suggest that class B1 GPCRs can form both homodimers and heterodimers, which may play that GLP-1R homodimerization occurs via transmembrane helix 4 (TM4), which forms the interface for both result, dimerized SecR receptors exhibit higher rates of G protein activation and release, improving both
- The Perils and Guardrails of Modifying Signalling Proteins in Bioassays
Dr. previously developed to bind Gαs in complex with active GPCRs, enabled detection of GLP-1R activation both
- Co-activation of GPCRs facilitate GIRK-dependent current
October 2022 "The activity of dopamine neurons is dependent on both intrinsic properties and afferent applications of sub-saturating concentrations of agonists where the co-application of one agonist resulted in both results suggest that the cooperative interaction between G βγ subunits and GIRK channels determines both Coincident activation of D2 and GABAB receptors leads to facilitation of GIRK channel currents, augmenting both
- Optimizing HTRF Assays with Fluorescent Ligands: Time-Resolved Fluorescence in GPCR Research
Measuring emission at both donor (usually 620nm) and acceptor (typically 665nm) wavelengths allows for Terbium is compatible with both red and green acceptors. expertise in GPCR biology with advanced fluorescence chemistry, Celtarys custom-developed ligands offer both
- Dimerization of GPCRs: Novel insight into the role of FLNA and SSAs regulating SST2 and SST5...
The cytoskeletal protein filamin A (FLNA) directly interacts with both somatostatin receptor type 2 ( A7), and octreotide but not pasireotide promoted hetero-dimerization in both A7 and M2 (+20.0 ± 11.8% On the contrary, in M2 cells, octreotide failed to internalize both receptors whereas pasireotide promoted In conclusion, we demonstrated that in GH3 cells SST2 and SST5 can form both homo- and hetero-dimers
- Isoforms of GPR35 have distinct extracellular N-termini that allosterically modify...
Additionally, we employed optical assays in living cells to thoroughly profile both GPR35 isoforms for basis for this bias, we examined structural models of GPR35 and conducted experiments with mutants of both found that a proposed disulfide bridge between the N-terminus and extracellular loop 3, present in both
- Lack of Oestrogen Receptor Expression in Breast Cancer Cells Does Not Correlate with Kisspeptin...
However, controversy remains regarding its role in breast cancer since both pro- and anti-metastatic We show that both cell lines express KISS1R mRNA and respond to KP-10 by elevating calcium mobilisation Interestingly, both cell lines displayed different complements of β-arrestin 1 and 2 expression.
- Nanobodies as Probes and Modulators of Cardiovascular G Protein-Coupled Receptors
single-domain antibody fragments from camelids, have become indispensable tools for interrogating GPCRs both technologies to discover nanobodies with tailored specificities may expand the impact of these tools for both


















