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October 2022 "Lysosomes coordinate cellular metabolism and growth upon sensing of essential nutrients, including cholesterol. Through bioinformatic analysis of lysosomal proteomes, we identified lysosomal cholesterol signaling (LYCHOS, previously annotated as G protein-coupled receptor 155), a multidomain transmembrane protein that enables cholesterol-dependent activation of the master growth regulator, the protein kinase mechanistic target of rapamycin complex 1 (mTORC1). Cholesterol bound to the amino-terminal permease-like region of LYCHOS, and mutating this site impaired mTORC1 activation. At high cholesterol concentrations, LYCHOS bound to the GATOR1 complex, a guanosine triphosphatase (GTPase)-activating protein for the Rag GTPases, through a conserved cytoplasm-facing loop. By sequestering GATOR1, LYCHOS promotes cholesterol- and Rag-dependent recruitment of mTORC1 to lysosomes. Thus, LYCHOS functions in a lysosomal pathway for cholesterol sensing and couples cholesterol concentrations to mTORC1-dependent anabolic signaling." Read more at the source #DrGPCR #GPCR #IndustryNews

At CA1-subicular presynaptic terminals 5-HT1B and GABAB receptors colocalize.

Subsequent experiments using primary astrocyte cultures revealed that Gi -DREADD stimulation significantly of the astrocytic Gi pathway attenuated intracellular calcium transients triggered by LPS treatment, suggesting

Crystal structures suggest ligand access to the orthosteric binding site of MT1 and MT2 receptors through The side-chain flexibility of Tyr5.38 was significantly different in the two receptor subtypes, as assessed Our simulations also suggest that the open state of Tyr5.38 generates a small pocket on the surface of

Neuronal Gα subunits required for the control of response to polystyrene nanoparticles in the range of

Many cause receptor misfolding and failure to reach the cell surface. that engage nascent mutant GPCRs in the endoplasmic reticulum, stabilizing folding and "rescuing" cell surface We previously demonstrated rescue of cell surface expression of luteinizing hormone receptor mutants Cell surface expression was severely reduced to ≤18% of wild-type (WT) for 11, modestly reduced to 66% of certain mutant FSHRs with severely reduced cell surface expression.

intracellular context ("in-cell") or those focused on characterizing molecules or events at the cell surface some key NMR techniques applied for on-cell NMR studies through both solution- and solid-state NMR and survey focus on the application of on-cell NMR spectroscopy to characterize ligand interactions with cell surface We also provide a brief survey of the applicability of on-cell NMR approaches to other classes of cell surface molecules.

present study examined the interaction between D2 and GABAB receptors using transient applications of sub-saturating heterologous facilitation was modelled based on the known cooperative interaction between the G protein βγ subunits The results suggest that the cooperative interaction between G βγ subunits and GIRK channels determines

The TAS1R2 and TAS1R3 subunits are members of a small family of class C GPCRs whose members share the TAS1R2 contains the primary binding site for most of the sweet-tasting compounds, including natural sugars ligand affinities of hTAS1R2-VFT were drastically reduced through the introduction of single amino acid substitutions

This review focuses on the role of neuropeptides in maintaining the homeostasis of the ocular surface

August 2022 Addex and Indivior Extend GABAB Positive Allosteric Modulator Research Collaboration for Substance agreement with Indivior PLC (LON: INDV) for discovering and developing novel oral gamma-aminobutyric acid subtype

. ✅ This is where survival is decided. Early-stage biotech hiring is not about perfect resumes. They are never sufficient. that survival traits are not abstract qualities. Survival traits determine whether anything gets done when they are not. How Founders Can Hire for Survival Without Overengineering It 👉 Once founders recognize that survival

The difference between surviving and failing in biotech is rarely science. Teams are no longer sure what success looks like. 👉 No single decision breaks the company, but the absence Teams that regain control do not suddenly become more confident about biology. Founders who succeed understand that strategy is not a one-time exercise. Instead of letting chaos accumulate quietly, they surface it early.

Biotech fundraising has undergone a subtle yet significant shift. What investors are really assessing is how clearly intellectual property supports the business being Slides list filings and dates, but do not explain how those rights support the fundraising narrative It fails when intellectual property does not clearly support the business being built.   . 👉 Founders who raise successfully treat intellectual property as part of their core narrative.

. 👉 When your cadence is unstable: Timelines slip quietly Dependencies surface late Teams optimize for activity, not momentum Scientific surprises hit harder because the system has no buffer ✅ What “good ✅ A stable cadence doesn’t eliminate surprise. It eliminates blindness .

Premium Sneak Peak:  Human Substance P–NK1R interactions observed by NMR; Endocrine Metabolic GPCRs 2026 Design GPCR binding affinity experiments that tell the truth , ensuring affinity data support—rather A quick rating on Spotify or Apple Podcasts — and a YouTube subscribe — helps us reach more scientists Beyond access, Premium sustains the nonprofit mission behind Dr. GPCR—supporting open resources while giving members deeper insight and earlier visibility.

The danger is subtle: 👉Scientific isolation feels busy, intelligent, respectable. But strategically, it’s suffocating.

Tracers bind not only to receptors but also to surfaces and unwanted proteins; non-specific binding must Proteins are not inert surfaces, and orthosteric binding reactions often continue beyond the first encounter This frequently masquerades as: Two binding sites Multiple receptor subtypes Allosteric modulation But Small differences produce subtle curvature; large differences produce biphasic behavior. Non-specific binding control:  Adsorption to surfaces changes free ligand concentration.

mindset and tactics he’s used for years—including the exact line that makes intimidating conversations surprisingly

No loud red flags.Just a series of subtle but firm questions pointing to what’s missing . Clarity, not complexity, is what makes approval possible, and biotech sustainable. 5️⃣ Patient targeting rationale: Are you selecting the right patient subgroup with a clear justification Building FDA-Ready Thinking into Your Strategy Regulatory success is not a function. If you can’t see them too, you’re not building strategy, you’re building surprises.

Subcellular membrane mixtures, altered receptor conformations, and non-specific interactions introduce events under near-physiological conditions while simultaneously generating image-based evidence to support localization, membrane composition, and intracellular trafficking states influence ligand binding in subtle , fluorescent tracers such as CELT-331 can report on ligand competition events directly at the cell surface Notably, no compound displayed toxicity or morphological changes at this concentration, supporting the

They could be engineered to target surface-exposed receptors, remain stable across batches, support live-cell imaging, and tolerate super-resolution workflows. Designing Reliable GPCR Imaging Tools for Real Biological Systems Success brought new challenges. The payoff was substantial. These optimizations enabled dual-color labeling strategies, surface-selective imaging, and ultimately

probes—designed with precise synthetic logic—enable deeper insight into GPCR internalization, trafficking, and surface What You’ll Learn Why peptide–fluorophore probes succeed where antibodies fail How parallel synthesis & testing accelerates probe optimization How surface-exposed receptor pools reshape interpretations of Help us reach more scientists by providing quick rating on Spotify or Apple Podcasts — and a YouTube subscribe GPCR is a 501(c)(3) non-profit organization—your participation directly supports our mission to advance

And they avoid the costly surprises that appear when in vitro conclusions collide with human physiology These nonlinearities matter: Competitive inhibition decreases as substrate increases. Uncompetitive inhibition strengthens as substrate increases—opposite of intuition. A compound may appear benign with one substrate and problematic with another. Kenakin reveals  the substrate strategy needed for credible DDI assessment.

It’s survival. Suddenly, the anomalies aligned.

The resulting multiparametric datasets are well-suited for GPCR research, where receptor trafficking, For GPCR assay developers, HCS supports:  Quantitative visualization of receptor internalization and Assay Design and Pilot Optimization Successful HCS begins with a clearly defined biological question Probe panels—such as lysosomal dyes or cytoskeletal markers—can be integrated to support multiplexed At Celtarys, we remain committed to enabling this transition and supporting researchers as they design

Scientific progress doesn’t guarantee startup success; strategic clarity does. By the time it surfaces, you’ve lost two months of budget and alignment. 2️⃣ Milestone redefinition Most biotech founders don’t suffer from having the wrong people. They suffer because everyone has a different idea of what their role actually is.   And suddenly, it becomes obvious what to kill and what to scale. ✅ That’s the power of strategic realignment

Watch Episode #177 The Experiment That Was Never Meant to Succeed When David Hodson’s lab teamed up with visualization tool Impact:  Shared widely → now used globally to map GPCR activity in live systems The success peripheral contributions to metabolic therapy Guide how next-generation incretin drugs are designed Support

Surgery electives meant long nights, constant patient responsibilities, and unpredictable call schedules For Hodson, one sustained curiosity thread involved a protein released by alpha cells in the pancreas Suddenly, the puzzle snapped into place. A long-running side project became a central insight.

Others show subtle curvature or slope deviations. It ’s a screening tool, not a substitute for rigorous Schild validation. Common revelations include: Mixtures of receptor subtypes  producing hybrid response patterns.