How do GRK-specific phosphorylation barcodes influence β-arrestin binding to GPCRs? New cryo-EM structures from Chen et al. (Nature, 2025) reveal that β-arrestin1 and β-arrestin2 form distinct complexes with ACKR3 depending on whether it's phosphorylated by GRK2 or GRK5, shaping arrestin conformation, complex stability, and engagement mode. Surprisingly, arrestin’s finger loop didn’t dive into the receptor core. Instead, it latched onto the micelle surface, breaking canonical expectations. Also, β-arrestin2 lacks a membrane anchor, making it more dynamic — a potential clue to its functional specialization. These findings underscore how barcode location + arrestin isoform = unique signaling outcomes.

 Read the full study: Inside Out: Mapping GPCRs from Membrane Codes to Market Moves

#GPCRs #Arrestin #ACKR3 #GRKs #CryoEM #StructuralBiology #SignalingBias #Phosphorylation #DrGPCR

Forget one receptor at a time. Go big.Ep.167 of the Dr.GPCR Podcast with Tom Sakmar & Ilana Kotliar is about scaling GPCR research with multiplexing, miniaturization, and collaboration. The tools are built. The data is free. What will you ask next?

📲 Dive in: Ep 167 with Drs. Tom Sakmar & Ilana Kotliar  

#GPCRtraining #GPCRresearchcommunity #DrGPCR #GPCRdata

We’re proud to welcome Celtarys as our media partner! Known for their fluorescent ligand innovation, Celtarys is helping researchers make biology visible, faster, smarter, and with more precision. Their chemistry speaks the language of biology, and now, they’re speaking to the global GPCR community through this powerful collaboration.

🔗 Explore Celtarys on the Dr. GPCR Ecosystem: https://www.ecosystem.drgpcr.com/celtarys-research-dr-gpcr-ecosystem

#DrGPCR #GPCRtools #FluorescentLigands #BiotechInnovation

Autoantibodies that activate GPCRs? Wild—but real. Tom Sakmar & Ilana Kotliar break down the link between GPCR autoantibodies, long COVID, and disease signaling in Ep.167 of the Dr.GPCR Podcast This episode is a must if you're thinking diagnostics.

📲 Tap to listen: Ep 167 with Drs. Tom Sakmar & Ilana Kotliar 

#GPCRautoantibodies #GPCRdrugdiscovery #DrGPCR #Immunology

We’re excited to announce our strategic partnership with Celtarys Research, a biotech company specializing in fluorescent ligand technologies and real-time, non-radioactive GPCR assays.

This collaboration combines Dr. GPCR’s global platform with Celtarys’ innovative chemical biology tools, making it easier than ever for scientists to study ligand-receptor interactions, visualize binding, and accelerate drug discovery.

We’re proud to welcome Celtarys to the Dr. GPCR ecosystem to support researchers worldwide and expand access to high-performance tools for GPCR-targeted therapeutics.

✳️ Read the complete press release: https://www.ecosystem.drgpcr.com/post/dr-gpcr-and-celtarys-research-join-forces-to-expand-access-to-innovative-gpcr-tools 

#GPCR #DrGPCR #CeltarysResearch #DrugDiscoveryTools #FluorescentLigands #GPCRresearch #ScientificPartnership

Class B GPCR drugs are reshaping treatment for migraine, diabetes, and obesity- but did you know ligand bias plays a key role in their success? This new review explores how tweaking peptide drugs can boost efficacy, reduce side effects, and unlock next-gen therapies.

Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox

➡️ https://www.ecosystem.drgpcr.com/reviews/where-are-we-now%3F-biased-signalling-of-class-b-g-protein-coupled-receptor-targeted-therapeutics 

#gpcr#drgpcr

220 GPCRs. One platform. Endless questions.

In Ep.167 of the Dr. GPCR Podcast, Tom Sakmar and Ilana Kotliar reveal a full GPCR-RAMP interaction map—powered by Luminex, dual-tagged constructs, and open science. Big win for the GPCR community.

✳️ Listen now: Ep 167 with Drs. Tom Sakmar & Ilana Kotliar 

#GPCRresearch #DrGPCR #GPCRpodcast #GPCRtools #OpenScience

What if you could map GPCR-RAMP interactions across the entire superfamily in a single experiment? That’s precisely what Dr. Kotliar from the Sakmar lab made possible!

In Ep.167 of the Dr. GPCR Podcast, we chat with Drs. Tom Sakmar and Ilana Kotliar about how their lab developed:

• A multiplexed Luminex assay to screen hundreds of interactions at once

• A 220-clone DUET-tagged GPCR library, available on Addgene

• An online interface to search GPCR-RAMP data and antibody validations

This is open-access science at its best, built for the GPCR research community.

✳️ Listen to the episode: Ep 167 with Drs. Tom Sakmar & Ilana Kotliar

#GPCRresearch #DrGPCRecosystem #GPCRdrugdiscovery #GPCRtrainingprogram #GPCRpodcast

How do GPCRs sense pH changes? New cryo-EM structures of GPR4 and GPR68 reveal how extracellular histidines act as proton sensors-trigger activation and biased G protein coupling!

Did you know that we work hard to bring you the most recent GPCR News, weekly?

Catch up today in the Ecosystem using your free site membership!

➡️ https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/structural-basis-and-biased-signaling-of-proton-sensation-by-gpcrs-mediated-by-extracellular-histidine-rearrangement 

#gpcr#drgpcr

Ben Clements reveals a 10x improvement in efficacy using GPCR-targeted PAMs, in Ep.166 of the Dr.GPCR Podcast,. The catch? It’s all about understanding the system, not replacing it.

From neuromas to novel modulators, this episode is full of breakthroughs that matter for patients.

📲 Watch now: Ep 166 with Dr. Ben Clements  

#GPCRresearch #DrGPCR #GPCRpodcast #OpioidPharmacology #DrugDiscovery

“Research is all about knowing when to walk and when to run.” –Ben Clements

In Ep. 166 of the Dr.GPCR Podcast, hear how a postdoc is reshaping the conversation on opioid use, imposter syndrome, and the power of collaborative science.

Why early-career voices are critical in GPCR drug discovery —and how lab culture makes all the difference.

🎧 Watch here: https://buff.ly/Kr3qKud

#GPCRresearch #DrGPCR #GPCRpodcast #OpioidPharmacology #DrugDiscovery

Did you know that certain ergot derivatives can produce wash-resistant signalling through the 5-HT2B receptor persisting for many hours without losing potency or efficacy? By using signalling assays, radioligand binding assay, and microscopy, Gaidarov et al. suggested that this phenomenon results from persistently/irreversibly internalised signalling receptor complexes.

Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! 

➡️ https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/mechanisms-of-constitutive-and-agonist-induced-5-ht2b-internalization%2C-persistent-endosomal-signaling-and-paradoxical-regulation-of-agonist-pharmacology

#gpcr#drgpcr

🔍 Running a GPCR lab? Applying for grants? Launching a nonprofit?Ep.165 of the Dr.GPCR Podcast is your finance + operations crash course—delivered by two experts who support early-stage mission-driven teams like Dr. GPCR.

🎧 Smart, practical, and full of real talk: Ep 165 with Chuck DeWeese & Joe St. Germain

#gpcr #DrGPCR #ScienceStartup

Can we preserve opioid pain relief without the side effects? 🔬

On Ep.166 of the Dr.GPCR Podcast, Ben Clements shares how positive allosteric modulators (PAMs) at the mu-opioid receptor could revolutionize treatment —with a 10x boost in methadone efficacy.

Tune in for a masterclass on translational pharmacology, curiosity-driven science, and meaningful mentorship.

🎧 Full episode: Ep 166 with Dr. Ben Clements 

#GPCRresearch #DrGPCR #GPCRpodcast #OpioidPharmacology #DrugDiscovery

Can we preserve opioid pain relief without the side effects? 🔬

On Ep.166 of the Dr.GPCR Podcast, Ben Clements shares how positive allosteric modulators (PAMs) at the mu-opioid receptor could revolutionize treatment —with a 10x boost in methadone efficacy.

Tune in for a masterclass on translational pharmacology, curiosity-driven science, and meaningful mentorship.

🎧 Full episode: Ep 166 with Dr. Ben Clements 

#GPCRresearch #DrGPCR #GPCRpodcast #OpioidPharmacology #DrugDiscovery

Disrupting VIPR2 dimerisation halts breast cancer spread—could TM3-4 peptides be the next breakthrough in targeted cancer therapy?

Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! 

➡️ https://www.ecosystem.drgpcr.com/gpcrs-in-oncology-and-immunology/dimerisation-of-the-vip-receptor-vipr2-is-essential-to-its-binding-vip-and-g%CE%B1i-proteins%2C-and-to-its-functions-in-breast-cancer-cells 

#gpcr#drgpcr

What do mission-driven teams and world-class science have in common? 

✅ Integrity 

✅ Systems that last

✅ The right people

In this episode, Joe & Chuck from Company Launch Partners share what it means to build something that endures.

🎧 Catch the full episode: Ep 165 with Chuck DeWeese & Joe St. Germain

#gpcr #DrGPCR #ScienceStartup

A high-resolution deep mutational scan of MC4R reveals how thousands of genetic variants impact obesity-linked signaling pathways and highlights new opportunities for precision drug discovery

Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox

➡️ https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/high-resolution-deep-mutational-scanning-of-the-melanocortin-4-receptor-enables-target-characterization-for-drug-discovery 

#gpcr#drgpcr

"Solving financial puzzles feels just like solving scientific ones," says Joe St. Germain from Company Launch Partners.Behind every successful research organization, there is a rock-solid operations team. Don’t miss this rare conversation bridging science, structure, and strategy with Chuck DeWeese & Joe St. Germain.

✳️ Tune in now: Ep 165 with Chuck DeWeese & Joe St. Germain 

#gpcr #DrGPCR #ScienceStartup

🚀 Science and finance aren't opposites—they’re partners.

In this Ep.165 of the Dr.GPCR Podcast, Joe St. Germain & Chuck DeWeese reveal what it really takes to build sustainable startups and nonprofits behind the scenes.

Grant accounting, character-first hiring, mission-driven growth—it’s all here!

🎧 Listen now: Ep 165 with Chuck DeWeese & Joe St. Germain 

#gpcr #DrGPCR #ScienceStartup