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September 2022 GPCR/endocytosis/ERK signaling/S2R is involved in the regulation of the internalization Our results showed that the inhibition of cellular respiration hindered the internalization of F-Hst1 Overall, phagocytosis, CME, GPCR, ERK signaling, and S2R/TMEM97 are involved in the internalization of The inhibition of either internalization or mitochondria-targeting of Hst1 could significantly compromise

This lesson reframes enzyme interaction not as background noise, but as a core pharmacological event. And responsible for countless drug–drug interactions. When Inhibition Becomes Activation Not all enzyme interactions are suppressive. Kenakin Content trusted by biotech, pharma, and academia 💎 $2999/year — one conference cost = a full Kenakin with your own enzyme or GPCR interaction puzzles.

We are able to identify the interaction of membrane cholesterols with definite sites and domains within We show that cholesterol interactions with the transmembrane domain TMD, unlike those with the cysteine-rich Notably, a few persistent interactions of cholesterol with lower TM cholesterol-binding domains are governed We have also reported the interaction of phosphatidylinositol 4-phosphate with the intracellular region The movement of these TM helices could possibly be a consequence of interactions involving the extracellular

August 2022 A new Kunitz-type snake toxin family associated with an original mode of interaction with and non-active V2R Kunitz peptides highlighted five positions, among which four are involved in V2R interaction We finally determined that eight positions, part of these two loops, interact with the V2R.

September 2022 CCL25/CCR9 interaction promotes the malignant behavior of salivary adenoid cystic carcinoma signaling pathway "Background CC chemokine receptor 9 (CCR9), an organ-specific chemokine receptor, interacts Western blot and RT–qPCR assays were carried out to measure the downstream factors of the interaction

Multiple 14-3-3 isoforms exist, and a GPCR can differentially interact with different 14-3-3 isoforms

GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health

G protein-coupled receptor interactions and modification of signalling involving the ghrelin receptor 1a (GHSR1a) is intriguing because of its potential as a therapeutic target and its diverse molecular interactions In all cases, the receptor interaction changes downstream signalling and the responses to receptor agonists

resonance (NMR) spectroscopy allows the determination of atomic-level information on intermolecular interactions In particular, we focus on the application of on-cell NMR spectroscopy to characterize ligand interactions

This is a highly prestigious international award – exemplified by the fact that other winners this year are the co-founders of BioNTech for their invention of the (Pfizer) Covid vaccine."

We uncovered a novel neuroprotective mechanism involving interaction between neurotrophic factor-α1 ( Co-immunoprecipitation and pull-down assays confirmed interaction between NFα1/CPE and 5-HTR1E and 125I Molecular dynamics studies revealed that NF-α1/CPE interacts with 5-HTR1E via 3 salt bridges, stabilized Thus, NF-α1/CPE uniquely interacts with serotonin receptor 5-HTR1E to activate the β-arrestin/ERK/CREB

This Week’s GPCR Intelligence: From Set-Point Pharmacology to No-Wash Internalization Assays This week Upcoming events:  47th Symposium on Hormones & Cell Regulation; new approach to GPCR internalization Target protected agonism:  Internalized MT2 signaling escapes AGRP antagonism—unlike α-MSH. GPCR scientists, translational pharmacologists, biotech discovery teams, and decision-makers who need tools, translational strategy, classified updates, and curated jobs—trusted by scientists, teams, and biotech

When pharmacologists misinterpret how an antagonist interacts with its receptor, the consequences ripple

βarrs) play multifaceted roles in the function of G protein-coupled receptors (GPCRs). βarrs typically interact However, the effects of the C tail- and TM core-mediated interactions on the conformational activation Here, we show the conformational changes for βarr activation upon the C tail- and TM core-mediated interactions Our NMR analyses demonstrated that while the C tail-mediated interaction alone induces partial activation exists in equilibrium between basal and activated conformations, the TM core- and the C tail-mediated interactions

Itch receptor MRGPRX4 interacts with the receptor activity-modifying proteins (RAMPs). Dopamine Receptor D1R and D3R and GRK4 Interaction in Hypertension. Therapeutics Reports Fourth Quarter and Full Year 2022 Financial Results and Recent Highlights Salipro Biotech Expansion of precision oncology pipeline announced by Exscientia Upcoming start-up ecosystem - leadXpro and InterAx (April 20 - 21, 2023) Swiss Biotech Day (April 24 - 25, 2023) SLAS Europe 2023 Conference and Exhibition

A Gαs preferentially interacts with dimeric β2-AR, but not monomeric β2-AR, in a resting state, resulting

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In this podcast, he lays out the mindset that helped shape products used across biotech and academia—and That opened the door to something rare in functional pharmacology: plate-based GPCR internalization tracking The Endogenous Receptor “Aha” Eric’s second “aha” moment with pHSense came the day his team showed internalization their native, unmodified state—unlocking new questions about constitutive activity, agonist-induced internalization teaming, testing, and failing smarter. 🚀 Why This Matters: Whether you’re launching a tool, starting a biotech

If you’re in GPCR discovery or biotech R&D, this is a masterclass in turning deep science into scalable failed in plate readers—too noisy, too dim. pHSense rewrote that rule, enabling high-throughput GPCR internalization Internalization as a Functional Readout The insight? GPCR internalization isn’t just a trafficking readout—it’s pharmacology. moment came when they ran a dose-response with Exendin-4 on GLP-1 receptors—and saw clean, plate-based internalization

When the biotech world gathers in Boston, this is where the real conversations begin. Every September, Boston welcomes the global biotech and drug discovery community. Why It Matters Connect with peers across biotech, CROs, and investment who are driving discovery forward Meet both the global biotech community and Boston’s local innovators in one room Be part of Dr. Our mission is simple: bridge science and industry  by connecting researchers, biotech, CROs, and pharma

Eric Trinquet, that moment arrived when his team successfully tracked GPCR internalization in native What if you could directly measure receptor internalization in physiologically relevant cells without These probes become brighter and have a longer lifespan as internalized receptors enter acidic endosomes—translating presented a data set that transformed everything: a clean, dose-dependent response of GLP-1 receptor internalization For the first time, a team demonstrated high-throughput internalization data in physiologically relevant

In practice, these criteria test the purity of interaction.

activation of the β2-adrenoceptor (β2AR) causes its S-nitrosylation that is required for the receptor to internalize

October 2022 "Neisseria meningitidis is a Gram-negative opportunistic pathogen that is responsible for causing human diseases with high mortality, such as septicemia and meningitis. The molecular mechanisms N. meningitidis employ to manipulate the immune system, translocate the mucosal and blood-brain barriers, and exert virulence are largely unknown. Human-associated bacteria encode a variety of bioactive small molecules with growing evidence for N-acyl amides as being important signaling molecules. However, only a small fraction of these metabolites has been identified from the human microbiota thus far. Here, we heterologously expressed an N-acyltransferase encoded in the obligate human pathogen N. meningitidis and identified 30 N-acyl amides with representative members serving as agonists of the G-protein coupled receptor (GPCR) S1PR4. During this process, we also characterized two mammalian N-acyl amides derived from the bovine medium. Both groups of metabolites suppress anti-inflammatory interleukin-10 signaling in human macrophage cell types, but they also suppress the pro-inflammatory interleukin-17A+ population in TH 17-differentiated CD4+ T cells." Read more at the source #DrGPCR #GPCR #IndustryNews

Corner delivers this week: high-impact insight into GPCR allostery, crafted for pharmacologists and biotech nuance into better decision-making. 🔍 This Week in Premium: Sneak Peek Industry insights:  Strategic biotech What you’ll learn: Reveal cryptic binding sites and time-dependent interactions.   This is where funders, peers, and biotech scouts are watching. GPCR scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who

We have previously shown interaction between PKR2 and anosmin 1 in vitro.

C5a is established to interact with a set of genomically related transmembrane receptors, like C5aR1 In addition, the structure of C5aR2 and its interaction specificity toward C5a is not structurally elucidated dynamics data presented in the current study are expected to further enrich the understanding of C5a-C5aR2 interaction

I call it the Lego Bucket Problem : You’ve got CRO output, internal assay data, maybe even some promising Hidden Cost of Good Science Without Systems I’ve seen this pattern again and again—across academia, biotech This is embedded consulting for biotech and VC teams who need to move fast —without compromising scientific Who I Work With ✅ Biotech Teams  – Especially those lacking in-house GPCR leads or overwhelmed by CRO assets in their portfolio. ✅ Contract Research Organizations (CROs)  – Wanting to better align with biotech

Kotliar share how three decades of curiosity evolved into a tech-powered platform for mapping GPCR-RAMP interactions Explore this week’s research, tools, and biotech insights in one place.

Beyond Academia: Advising Biotech Carlsson’s collaborative philosophy has also found a place in the biotech It also allows Carlsson to stay plugged into the fast-changing needs of biotech while keeping his academic Whether in academia or biotech, the future belongs to research groups that can orchestrate ecosystems And for the next generation of researchers and biotech leaders, that is the real collaboration advantage