Aberrant hormone receptors regulate a wide spectrum of endocrine tumors Aberrant G-protein coupled receptor (GPCR) expression is highly prevalent in cortisol-secreting primary bilateral macronodular adrenal hyperplasia (PBMAH) and unilateral adenomas. The aberrant express...

Aberrant or ectopic hormone receptors and their ligands play a much wider role than appreciated in regulating hormonal secretion via endocrine, paracrine, and autocrine modes in many #endocrine #tumours thelancet.com/journals/lan...
#GPCRs

#MedSky #EndoSky #OncSky

Welsh firm Antiverse raises funds for AI antibody platform Cardiff's Antiverse has raised $9.3m to develop its AI-based design platform for antibodies against hard-to-reach targets like GPCRs and ion channels.

#Antiverse #AI #AIantibodyplatform #biotech #drugdiscoveryprogrammes #antibodybasedtherapeutics #antibodies #drugtargets #Gproteincoupledreceptors #GPCR #ionchannels #NxeraPharma #GPCRs #cellularcommunication #transmembraneprotein #Tcellreceptor #TCR #antiPD1antibodies #drugdiscovery
zurl.co/cAKcg

If you're at the Endocrine Metabolic GPCRs 2026 meeting in Liverpool, UK, this week, why not say 'hello' to Hello Bio! 👋

You'll find James in the exhibition space today and tomorrow - he looks forward to meeting you 😊

#endocrine #endocrinemetabolic #gpcr #GPCRs #endocrinology #metabolism

Immunomodulation of Proton-activated G Protein-coupled Receptors in Inflammation

This review explores proton‑activated #GPCRs, pH‑sensing receptors that modulate #ImmuneResponses, highlighting their roles in #InflammatoryDiseases and future directions for understanding immune regulation under pathological conditions.
Read: doi.org/10.1007/s115...

Prof. Yuanchao Wang team at Nanjing Agricultural University #NAU developed the #toGC: A pipeline to correct #gene model for functional excavation of dark #GPCRs in #Phytophthora sojae
❇️https://doi.org/10.1016/j.jia.2024.03.077
@keaipublishing.bsky.social

Aberrant hormone receptors regulate a wide spectrum of endocrine tumors Aberrant G-protein coupled receptor (GPCR) expression is highly prevalent in cortisol-secreting primary bilateral macronodular adrenal hyperplasia (PBMAH) and unilateral adenomas. The aberrant express...

Regulation of #endocrine #tumours by aberrant GPCR is not restricted to cortisol-secreting adrenal lesions, but also occurs in tumours of several other organs www.thelancet.com/journals/lan...
G-protein coupled receptors #GPCRs

Insights into the Mechanism of Action of Tirzepatide: A Narrative Review - Diabetes Therapy Tirzepatide is the first dual long-acting glucose-dependent insulinotropic polypeptide receptor and glucagon-like peptide-1 receptor agonist indicated for the treatment of type 2 diabetes in adults, f...

📈 This matters now more than ever. #GPCRs dominate today’s biggest therapeutic wins, most visibly in obesity, where how receptors are modulated drives both efficacy and tolerability.

link.springer.com/article/10.1...

Aberrant or ectopic hormone receptors and their ligands
play a much wider role than appreciated in regulating
hormonal secretion via endocrine, paracrine, and
autocrine modes in many endocrine tumours www.thelancet.com/journals/lan...
#GPCRs #endocrine #tumours

#MedSky #EndoSky #OncSky

Proposed mechanism of receptor-dependent activity of bitopic ligands. Structures of PTHR1 and A2AR used in this panel were generated using Alphafold2.

Bitopic ligands comprise a #pharmacophore & a linked moiety that bind to separate sites. @rche54.bsky.social &co show that #GPCRs that bind small molecules can be potently activated by #bitopic #nanobody -ligand conjugates to selectively target pairs of GPCRs @plosbiology.org 🧪 plos.io/4p3VOyH

Proposed mechanism of receptor-dependent activity of bitopic ligands. Structures of PTHR1 and A2AR used in this panel were generated using Alphafold2.

Bitopic ligands comprise a #pharmacophore & a linked moiety that bind to separate sites. @rche54.bsky.social &co show that #GPCRs that bind small molecules can be potently activated by #bitopic #nanobody -ligand conjugates to selectively target pairs of GPCRs @plosbiology.org 🧪 plos.io/4p3VOyH

Proposed mechanism of receptor-dependent activity of bitopic ligands. Structures of PTHR1 and A2AR used in this panel were generated using Alphafold2.

Bitopic ligands comprise a #pharmacophore & a linked moiety that bind to separate sites. @rche54.bsky.social &co show that #GPCRs that bind small molecules can be potently activated by #bitopic #nanobody -ligand conjugates to selectively target pairs of GPCRs @plosbiology.org 🧪 plos.io/4p3VOyH

How molecular signaling bias can lead to better drug design About one-third of all drugs approved by the Food and Drug Administration target the largest family of cell membrane receptors called G protein-coupled receptors (GPCRs).

How molecular signaling bias can lead to better drug design. #physorg #GPCRs phys.org/news/2025-10...

We’re in Oxford today for the 1st UK Chemical Probes Hackathon! 🎯
Postdocs & PhD students join experts to assess GPCR probes and improve research quality.
Hosted by @ChemProbes + @UniofOxford
#ChemicalProbes #GPCRs #DrugDiscovery

Here's another important QSPainRelief publication about allosteric sites at #GPCRs: They can be identified by looking at how strongly certain receptor sites are coupled to #conformational changes that occur during activation.

🔗 doi.org/10.3390/ijms...

#allostery #pharmacology #receptors #ligands

🎯Feature Alert 🚨
This paper delves into how #BindingKinetics reshape our understanding of #allosteric modulation. When it comes to cooperativity effects, it's all about

👉 WHERE molecules bind
👉 HOW FAST
👉 and in WHICH SEQUENCE

🔗 doi.org/10.1016/j.dr...

#allostery #pharmacology #DrugDesign #GPCRs

🚀 Time-dependent #ligand-receptor #BindingKinetics and functionality in a #heterodimeric receptor model by Ortiz et al. (2024): Predicting how 2 drugs bind to a receptor complex over time - with implications for combination-therapies and #DrugDesign💊

🔗 doi.org/10.1016/j.bc...

#Pharmacology #GPCRs

We have a fabulous finish with @konjikusicmia.bsky.social (@reiterlab.bsky.social, UCSF) on #GPCRs, #signaling, and #hypogonadism in #BBS models across the hypothalamus-pituitary-gonad axes and its many ciliated cell types! #Ciliopathies? www.biorxiv.org/content/10.1... #UKCilia2025 /6

How do #fungi sense their #plant hosts?
This study shows host peroxidase triggers dimerization of two key F. graminearum GPCRs—FgSte2 & FgSte3—using BRET, pulldown assays, and microscopy 🧫🔬
A novel insight into ROS-driven fungal signaling!
Read it here 👉 buff.ly/GLgM1g1
#GPCRs #FungalPathogens

New research uncovers heterodimer formation between Fusarium graminearum #GPCRs FgSte2 & FgSte3 🧬
Using BRET, researchers show host peroxidases stimulate this pairing—advancing our understanding of fungal chemotropism & plant pathogenesis 🌾🍄
🔗 doi.org/10.1139/bcb-...
#FungalBiology #PlantPathology

Big news indeed 👏 make sure you check out the post&link below 🤩
#cryoEM #cryoET
#membraneproteins #GPCRs #scivis #scicomm

Welcome to the 49th FEBS Congress in Istanbul! 🎉 Starting with Dr. Beck-Sickinger on GPCRs & Dr. Hotamisligil on cell architecture & organelle function, plus Welcome Drinks! 😊 #FEBS2025 #GPCRs #CellBiology
See our Virtual Issue: febs.onlinelibrary.wiley.com/doi/toc/10.1...
@febspress.bsky.social

Very happy that this is now out. Cool collaboration with Weikert and Gmeiner group
#cryoem #gpcrs 🧪 @uni-wuerzburg.de @fau.de

Rhodopsin activation in lipid membranes entails a large influx of bulk water into the protein core. (A) Dark-state rhodopsin has a closed, dehydrated conformation of the 7-transmembrane helical bundle (30). (B) Open metarhodopsin-II conformation is adopted after retinal photoisomerization with outward-tilted TM6 (blue) and extended TM5 (green) helices following pH-dependent breakage of the Glu134–Arg135 salt bridge (31). (C) Large numbers of water molecules (~80–100) enter rhodopsin as determined by osmotic stress data for various-sized polyethylene glycols (PEGs). Smaller PEGs show smaller apparent water influx than more excluded large PEGs. The number of water molecules determined by the universal large osmolyte response is indicated by the dotted line. (D) Increase in virial coefficient ΔC for volume versus osmotic pressure accompanies rhodopsin photoactivation. Larger ΔC is determined in the exclusion limit of larger PEGs with the dotted line as the universal response. (E) Viewed from the intracellular side, dark-state rhodopsin is closed with residues colored by hydrophobicity (red, hydrophobic; white, hydrophilic). (F) The MII state shows an opened hydrophilic cavity (white) to accommodate the influx of bulk water which (G) widens as the C-terminal peptide of the G-protein (here Gi) is docked

💧🧬 Key drug targets in your body, the #GPCRs, need a massive influx of water to activate, even more than their size? Fried et al. found this and more. Dive deeper at doi.org/10.25422/azu... & doi.org/10.1073/pnas.... Image: Fried et al. (2022). CC BY-NC-ND 4.0
#OpenData #OpenScience #DrugDesign

How do #GPCRs traffic via the #ER and #Golgi to the #CellSurface—and what goes wrong in disease? ⚙️ Review by Assoumou et al: doi.org/10.1002/1873-3468.70081

😍 Lisa's sketch illustrates her passion for #GPCRs: Don't miss her most recent @chemicalscience.rsc.org 📜 publication about "Identification of allosteric sites and ligand-induced modulation in the dopamine receptor through large-scale alchemical mutation scan"🔗 doi.org/10.1039/D4SC... #compchem

Annette Beck-Sickinger now on stage — exploring peptide signaling and GPCR pharmacology with a focus on chemerin and its receptor system. From biased agonism to receptor trafficking, unveiling how peptides fine-tune cellular responses.
#CSSB25 #GPCRs #Chemerin #PeptideScience

A new study introduces the Gαi bONE-GO biosensor, a powerful tool for visualizing native GPCR signaling and uncovering hidden dynamics like partial agonism of opioid neuropeptides #Pain #GPCRs #Signaltransduction #GαibONE-GO www.science.org/doi/full/10....

Multi-pass #TransmembraneProteins are key drug targets, but their instability makes them tricky to work with. We offer solutions to improve stability and conformation.

Get up to 60% OFF on Claudins, #GPCRs, SLCs, and more! 👉https://ow.ly/aWyi50VO8bf