predicted that all the compounds showed the critical salt bridge with Glu172 with variable degrees of π-stacking

Perkins' Molecular Endocrinology and Pharmacology Laboratory team who are investigating new ways to tackle

diseases, but few therapies have been directed against GPCRs in the field of cancer, partly because of the lack

Effective methods to treat preeclampsia are lacking, and termination of pregnancy remains the only curative

A panel discussion will tackle best practices for measuring GPCR signaling bias in vitro and what that

They happen in the hallway between sessions, at the coffee station, or in the ten minutes after a talk It's the size where you can actually talk to everyone in the room. Where you walk away with a handful of connections that actually go somewhere, not a stack of business Their deorphanisation track record (17 identified natural receptor-ligand pairs) speaks to the depth

The panels are packed. Everyone’s rushing from one talk to the next. But the truth?

physiological and disease functions, yet knowledge of their role in colon cancer stem cell maintenance is still lacking

However, researchers faced a challenge with the target C5aR , as they lacked the appropriate tools to However, there is a notable lack of fluorescent probes available in the market for this receptor.

Procrastination may seem tempting, but tackling your work incrementally will save time and reduce stress

After a brief pause over the holidays and last month, we’re back in full force—designed to help you make

in endothelial cells, which was evidenced by the attenuation of organ fibrosis in mice specifically lacking

Currently-approved treatments have improved patient outcomes, but therapies to stop or reverse HF are lacking

The Era of Cold Fingers and Patience Back then, GPCR signaling experiments weren’t elegant; they were

It was supposed to be just a summer project—routine pipetting, repetitive assays, a box to tick before Many GPCR scientists trace their origin story back to a single unexpected spark. Not a grand plan.

extracellular N-termini by 31 amino acids, but detailed insights into their functional differences are lacking

This technique can acquire three-dimensional image stacks, facilitating the reconstruction of GPCR distribution If the experiment is done on live cells , tracking real-time receptor internalization becomes possible

His talk digs into the molecular basis of partial agonism at the mu opioid receptor, using mitragynine It is a timely look at how receptor pharmacology can sharpen one of the most talked-about therapeutic At Discovery on Target she is giving a talk on an NMR fragment screen against an orphan GPCR, describing Stepping into the GPCR track at Discovery on Target is part of that work. Inside the GPCR Track This Year The GPCR content is concentrated on Wednesday, September 30, and it spans

Welcome back GPCR Fans, Clean data can still mislead if the underlying assumptions aren’t tested.

With this high-resolution, dynamic view of GPCR activation, scientists can better tackle diseases by

We highlight this article by Tahk et al.  

Welcome back GPCR fans, If your drug discovery strategy still relies on static GPCR models, you’re already

stall not because the target is wrong—but because the chemical matter  interacting with that target lacks

To tackle these, the lab employs molecular docking, molecular dynamics simulations, and ligand-based

quantification of SST2/SST5 dimerization in rat GH3 as well as in human melanoma cells either expressing (A7) or lacking

And once you see it, you’ll never go back.

And once you make that shift, you’ll never go back.

It was mostly just because, I need to be back in the lab.”

β-arrestin readouts, the subtypes that matter for weight loss, and ortholog assays that tie bench data back

or pharmacological activation of endogenous Ca2+ signaling transducers; however, such approaches can lack