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Many GPCR scientists trace their origin story back to a single unexpected spark. Not a grand plan.

discovery: • Why Nature Was First : From opium to antibiotics, nature’s molecules still outperform many

Like many other organs, various GPCRs play a role in regulating liver function. the role of GPCRs in hepatic stellate cells (HSCs), the primary cells that regulate liver fibrosis, may

Many cause receptor misfolding and failure to reach the cell surface.

receptors (MCR3), as well as the MCR3 accessory protein, MRAP2, providing possible mechanisms for its many

Finally, we report that JQ1 treatment downregulated expression of many GPCRs and also impaired ERK1/2

That brought him to type 2 diabetes  — a condition affecting nearly every family, marked by social and The “Aha” Moment — Ten Years in the Making Many discoveries unfold slowly — dozens of experiments that

The Innovation Trap: Why Most Scientists Think Too Narrowly Eric doesn’t mince words: many junior scientists

Antibody batch-to-batch differences Antibodies from different lots may show different characteristics Specificity issues Some antibodies bind to shared epitopes across different proteins, which may lead Fluorescent ligands  provide some key advantages  that may solve these issues: 1.       interactions and signaling pathways. -            Biased signaling detection Biased pharmacophores may Charlottesville (VA): University of Virginia; [cited 2025 May 16].

Power analysis tells you exactly how many replicates you need for 95% confidence.

Find speaker details on the Live Talks page and mark your calendar HERE. extracellular calcium pathways Versatile lactate signaling via HCAR1: a multifaceted GPCR involved in many 2024 | Ligand Recognition and Molecular Gating Conference April 5 - 10, 2024 | AACR Annual Meeting May 13 - 17, 2024 | 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS

Fast forward to today: dozens of GPCR structures  exist, many in multiple conformations or bound to G

. 👉 Instead of shipping early and iterating, many scientific founders keep refining decks, processes

Earlier than many teams do.

The hypothesis arises that GPCR and β-arrestin-centered effector complexes vary based on subcellular For example, the binding sites for many β-arrestin interaction partners remain elusive, and certain effector proteins with overlapping sites may experience mutually exclusive binding due to steric hindrance (Crépieux Profiling Interactive Analysis (GEPIA) tool, it is evident that β-arrestin expression is dysregulated in many In certain cancer types, only one β-arrestin isoform's expression may be altered, while the other remains

But here’s the truth: too many programs still fail because early decisions were built on shaky mechanistic

The ratiometric readouts correct many inconsistencies such as pipetting errors. Curr Chem Genomics. 2009 May 28;3:22-32. doi: 10.2174/1875397300903010022.

GPCRs play a central role in neuronal signaling and have been used to treat these diseases with varying Over 30% of FDA-approved drugs target GPCRs, with many targeting CNS located GPCRs. The conformation change induced by the agonist may not always lead to the same intracellular signaling Studying these routes may reduce side-effects when using GPCR-based therapies.

Ignore these forces, and your “selective” agonist may deliver surprises the first time it meets a patient Volunteer Gap Many programs die in Phase II, not because the molecule is “bad,” but because its profile Get a sense of why inverse agonists may be necessary to truly shift the physiological balance.

Yet too many programs rely solely on affinity metrics—Kd—as proxies for in vivo behavior, missing a critical

The delisting dilemma: Why do so many biotechs face being kicked off the Nasdaq?. (May 22 - 26, 2023) 2nd LEAPS Meets Life Sciences Conference. (May 14 - 19, 2023) 8th and final ERNEST Meeting in Crete. (May 3 - 7, 2023).

by a single G protein-coupled receptor type (5-HT2A) GPCRs in Oncology and Immunology The power of many

This is the silent advantage of many successful drugs: they bind tightly or covalently , making target This PK/PD dissociation  means: Drug exposure may end, but receptor occupancy remains.

where different ligands acting on the same receptor trigger distinct signaling pathways, leading to varied Cary, B.P., et al., New Insights into the Structure and Function of Class B1 GPCRs.  

GPCRs pose a critical challenge in drug discovery: a vast therapeutic potential with many targets yet Br J Pharmacol. 2020 Mar;177(5):978-991. doi: 10.1111/bph.14953.

agonists of FFAR4 for type 2 diabetes mellitus therapy Industry News OMass Therapeutics Welcomes Melissa Faris Physiology Summit April 5 - 10, 2024 | AACR Annual Meeting April 22 - 23, 2024 | Endocrine Metabolic GPCRs May 13 - 17, 2024 | 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS

combines high-throughput DNA sequencing with systematic mutagenesis to create and assess the impact of many

Below is your Classified GPCR News at a glance for May 29th to June 4th, 2023. Activity Models of Key GPCR Families in the Central Nervous System: A Tool for Many Purposes.

For Carlsson, this marked a shift in how his lab approached GPCR research. Many of his former students now work in industry, where their ability to bridge the computational-experimental

The same compound may appear inactive in one substrate system, then wildly active in another. neurodegeneration, metabolic disease, and regenerative pharmacology—fields where fine-tuning enzyme behavior may Yet many discovery teams still relegate them to the “ADME” checklist, rather than the strategic design