📢 Call for papers | @FrontiersIn

"Rational Design of Peptide-Based Therapeutics for GPCRs"

We invite original research, reviews & perspectives — from #peptidechemistry and #GPCR biology to #drugdiscovery .

#Peptides #peptide-conjugates #Peptidomimetics

https://www.frontiersin.org/research-topics/74502/rational-design-of-peptide-based-therapeutics-for-gpcrs

"Evolving GPCRs activated by inert ligands."

📍Engineered receptors activate with clozapine-N-oxide
📍Validated in human cells
📍Facilitates specific signaling studies

#GPCR #CellBiology #Bioengineering #Pub2Post

https://tnyp.me/MXaHLYnS/m

Innovative GPCR design with inert activation:

🔑 Engineered GPCRs are activated by clozapine-N-oxide.
👨‍🔬 Validated in yeast and human cells.
🧪 Successfully expressed in human artery cells.
🔍 Proved valuable in neuronal studies.

#GPCR #DREADD #CNO #Pub2Post https://tnyp.me/kGMOwdqN/m

🧬 Can entropy help us decode how hormone receptors make real-time decisions?

🔗 Temporal complexity of LVV-hemorphin-7 allosterism at the angiotensin II type 1 receptor assessed using entropy-based approaches. Computational and Structural Biotechnology Journal, DOI: https://doi.org/10.1016/j.csbj.2025.10.024

📚 CSBJ: https://www.csbj.org/

#StructuralBiology #Biophysics #GPCR #Entropy #MolecularPharmacology #AllostericModulation #DrugDiscovery #MolecularDynamics

💊 Can understanding receptor bias help us design safer, more selective GPCR drugs?

🔗 Biased activation of the vasopressin V2 receptor probed by molecular dynamics simulations, NMR and pharmacological studies. Computational and Structural Biotechnology Journal, DOI: https://doi.org/10.1016/j.csbj.2024.10.039

📚 CSBJ: https://www.csbj.org/

#GPCR #StructuralBiology #MolecularDynamics #NMR #Pharmacology #ProteinStructure #DrugDiscovery #ComputationalBiology #CellSignaling

🍽️🧠 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: https://doi.org/10.1016/j.csbj.2024.11.035

📚 CSBJ: https://www.csbj.org/

#GPCR #GhrelinReceptor #StructuralBiology #MolecularDynamics #DrugDiscovery

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. #biotech #drugdevelopment #funding #GPCR #ionchannels

https://redrobot.online/2025/03/maxion-therapeutics-secures-e68-million-in-series-a-funding-for-antibody-based-drug-development/

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

🔗 https://doi.org/10.1016/j.str.2025.01.011

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

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

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

https://biorxiv.org/content/10.1101/2024.10.31.621373v1

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