#gpcr

CSBJcsbj
2025-10-02

🍽️🧠 What makes the ghrelin receptor so adaptable — controlling both hunger and memory at the molecular level?

🔗 An atomic look at the interface of GHSR and its partners. Computational and Structural Biotechnology Journal, DOI: doi.org/10.1016/j.csbj.2024.11

📚 CSBJ: csbj.org/

An atomic look at the interface of GHSR and its partners. Computational and Structural Biotechnology Journal, DOI: https://doi.org/10.1016/j.csbj.2024.11.035
2025-08-08

β-arrestins regulate #GPCR signaling & trafficking, adopting multiple conformational states with different outcomes. This study shows how receptor CXCR7 induces stepwise conformational changes in β- #arrestin 2, uncovering an arginine switch mechanism of activation @PLOSBiology plos.io/3UfTd71

Top left: Comparison of polar core and three-element interactions between the inactive and intermediate conformations of βarr2. The ribbon diagram of βarr2 is colored dark gray. C7pp2 and the C-tail of βarr2IM are shown in pink and green, respectively. Hydrogen bonds stabilizing the polar core interactions are shown as dashed lines. Top right: CXCL12-induced trafficking of βarr2 as monitored using confocal microscopy in HEK293 cells expressing CXCR7WT and CXCR7E358A. The “Surface” images depict βarr2 localization at the plasma membrane shortly after agonist stimulation, representing initial recruitment of βarr2 to CXCR7. The “Endosomal” images show intracellular βarr2 localization at later time points, indicating receptor internalization. Scale bar is 10 μm. Bottom: Proposed arginine switch model for βarr2 activation by the CXCR7 Rp-tail. In the inactive state, Arg394, which we name as an “arginine switch,” is an integral component of the polar core, facilitating interaction. Simultaneously, the βarr2 C-tail engages with the N-domain through a 3E interaction. Upon C7pp2 binding to βarr2, the arginine switch undergoes rotation and forms a direct interaction with Glu358 of C7pp2, leading to partial disruption of the polar core. This stage represents an intermediate state preceding βarr2 activation, where the 3E interaction remains intact. Phosphorylation of Ser360/Thr361 further contributes to the disruption of the 3E interaction, triggering the release of the βarr2 C-tail.
2025-03-18

Cambridge-based Maxion Therapeutics raises €68.9 million in Series A funding led by General Catalyst to advance its KnotBody pipeline targeting ion channel and GPCR-driven diseases.Maxion Therapeutics, a Cambridge-based biotech firm, has raised €68.9 million in a Series A funding round led by General Catalyst.

redrobot.online/2025/03/maxion

2025-02-09

"Direct effect of membrane environment on the activation of mGluR2 revealed by single-molecule FRET" in #Structure

🔗 doi.org/10.1016/j.str.2025.01.

🧵 #GPCR #mGluR🧼#detergents #cholesterol
🔬 #smFRET
💻🧪 #MD #mutants

Congrats to C. Banerjee, B. Liauw, and R. Vafabakhsh!

Emmanuel Margeatemargeat@mstdn.science
2024-11-06

Check our new preprint !
Triple orthogonal labeling with 2 unnatural aminoacids + 1 SNAP-Tag for 3 color #smFRET.
We resolve a new intermediate in the activation of metabotropic glutamate receptor 2.

#GPCR #clickchemistry

biorxiv.org/content/10.1101/20

Collaboration with Jean Philippe Pin & Philippe Rondard (IGF Montpellier) & Don Lamb (LMU Munich)

2024-06-21

Biophysicists at #UniLeipzig demonstrate mechanism of #signalling by adrenaline-binding #receptor at atomic level. In the future, researchers could use the results to avoid side effects when developing drugs.
#GPCR @SFB1423

nachrichten.idw-online.de/2024

Foto darf nur im Zusammenhang mit der Pressemitteilung verwendet werden.
2024-06-21

Biophysicists at #UniLeipzig demonstrate mechanism of #signalling by adrenaline-binding #receptor at atomic level. In the future, researchers could use the results to avoid side effects when developing drugs.
#GPCR @SFB1423

nachrichten.idw-online.de/2024

Foto darf nur im Zusammenhang mit der Pressemitteilung verwendet werden.
2024-06-21

Biophysiker der #UniLeipzig weisen Mechanismus der #Signalübertragung durch Adrenalin-bindenden #Rezeptor auf atomarer Ebene nach. Mit den Ergebnissen könnten Forschende künftig Nebenwirkungen bei #Entwicklung von Wirkstoffen umgehen.
#GPCR @SFB1423

nachrichten.idw-online.de/2024

Foto darf nur im Zusammenhang mit der Pressemitteilung verwendet werden.
2024-05-13

The version of record of our #Nematostella #GPCR #neuropeptide paper has now been published
elifesciences.org/articles/906

For #cnidarian #neuroscience there are lots of new deorphanised receptors described in the paper. We also identified orthologs across cnidarian species, including corals, #Exaiptasia etc. so the resource is not limited to Nematostella.

SEM image of a Nematostella planula larva. The larva is fully ciliated and has an apical tuft of long cilia.
2024-04-30

New study shows that the C-terminal fragment of the #GPCR #muscarinicM2receptor, translated from an #IRES, localizes to the #mitochondrial inner membrane & is upregulated upon stress exposure, reducing respiration & #ROS to protect cells #PLOSBiology plos.io/3Uomtb8

2024-02-26

For our #Nematostella neuropeptide-GPCR screen paper elifesciences.org/reviewed-pre, we have now published a detailed protocol here:
bio-protocol.org/exchange/prep
If you are interested in #GPCR #neuropeptide #pharmacology #cnidaria #neuroscience have a look!

A dose-response curve for a cnidarian GPCR receptor activated by various PRGamide neuropeptides.
🎃🐦‍🔥nemo™🦇 🇺🇦🍉nemo@mas.to
2024-02-25

#BC007 ist ein potenzieller Wirkstoffkandidat gegen das #PostCovidSyndrom und andere #Autoimmunkrankheiten mit funktionellen Autoantikörpern gegen #GProtein gekoppelte Rezeptoren #gpcr Es handelt sich um ein #aptamer das diese krankmachenden #Autoantikörper blockieren soll. Die klinische Phase-II-Studie reCOVer der Augenklinik des #Uniklinikums #Erlangen untersucht den molekularen Weg bestimmter Autoantikörper beim Post-COVID-Syndrom. In diesem Zusammenhang startet in …

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2023-12-15

Longhaulers should petition for access to this molecule. It will help. Very interesting the way it works. Both sources describe it better than I could myself, so I'll just point you in their direction.

Popular:
dicyt.com/viewNews.php?newsId=

In depth: researchgate.net/publication/2

#LongCovid
#C5a
#C5aInhibitor
#GPCR
#Covid

2023-12-07

The #GPCR CMKLR1 responds to the #adipokine #chemerin and is abundant in #InnateImmune cells. Structure of CMKLR1 in complex with #Gprotein and a peptide agonist (+ mutagenesis & simulations) reveals mechanisms of action #PLOSBiology plos.io/4a6Igvd

RCNS MedChem Research Groupkeserulab
2023-11-29

GproteinDb update brings new G protein- couplings, AlphaFold2-multimer models, interface interactions and coupling selectivity analysis
t.co/goZcFihoeX

2023-07-17

First preprint about my work at Schrödinger:

We show how to predict ligand efficacy via absolute binding free energy perturbation on different receptor conformations — confirming and utilizing the principle that the functional response of a receptor is mainly determined by the thermodynamics of ligand binding.

chemrxiv.org/engage/chemrxiv/a

#FEP #FreeEnergy #LigandEfficacy #GPCR #DrugDiscovery #DrugDesign #Thermodynamics #GPCRs #BindingFreeEnergy

2023-07-14

Our favourite #Platynereis #opsin now in the mammalian brain as a new #optogenetic tool!

"Here we ... found that the Platynereis dumerilii ciliary opsin ... is an efficient, versatile, light-activated bistable GPCR that can suppress synaptic transmission in mammalian neurons with high temporal precision in-vivo "

biorxiv.org/content/10.1101/20

#neuroscience #GPCR

Schematic representation of an autaptic neuron recorded in the whole-cell configuration. On the right, representative EPSCs traces evoked by a pair of 1 ms
depolarizing current injections in a PdCO-expressing autaptic neuron.

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