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Prostaglandin (PG) signaling regulates a wide variety of physiological and pathological processes, including Many G-protein-coupled receptors (GPCRs) including EP4 are localized in cilia for modulating cAMP signaling During development, PGE2 signaling regulates embryogenesis, hepatocyte differentiation, hematopoiesis This review outlines recent advances in understanding the functions and mechanisms of prostaglandin signaling

Rho1 signaling is activated by G-protein-coupled receptor (GPCR) signaling at the cell surface. embryonic salivary gland (SG) invagination, the GPCR ligand Folded gastrulation (Fog) activates Rho1 signaling The SG receptor that transduces the Fog signal into Rho1-dependent myosin activation has not been identified Here, we reveal that the Smog GPCR transduces Fog signal to regulate Rho kinase accumulation and myosin

Historically, drug discovery efforts targeting GPCRs focused on G-protein-dependent signaling pathways Extracellular signal-regulated kinases (ERK), a subset of the mitogen-activated protein kinase (MAPK) family, have long been known to play a critical role in the signaling pathways of GPCRs. This signaling cascade involves several steps. Biased receptor signaling in drug discovery. Pharmacological Reviews, 71(2), 267-315.

The Era of Cold Fingers and Patience Back then, GPCR signaling experiments weren’t elegant; they were Reading those first papers on GPCR signaling organization absolutely fascinated me — the idea that receptors What Changed After This : High-throughput capabilities meant researchers could map GPCR signaling more The field moved from single readouts to integrated signaling landscapes, accelerating drug discovery now it’s the foundation — a starting point for more ambitious questions about GPCR networks, biased signaling

Although they form an ancient signaling system, there is still a great deal of variety in neuropeptides Additionally, we discovered that the neuropeptide signaling systems of Sternorrhyncha were very different groundwork for the creation of novel D. vitifoliae management strategies that specifically target these signaling

Rho1 signaling is activated by G-protein-coupled receptor (GPCR) signaling at the cell surface. embryonic salivary gland (SG) invagination, the GPCR ligand Folded gastrulation (Fog) activates Rho1 signaling The SG receptor that transduces the Fog signal into Rho1-dependent myosin activation has not been identified Here, we reveal that the Smog GPCR transduces Fog signal to regulate Rho kinase accumulation and myosin

Using different optical biosensors to measure the activation of PTH1R and its downstream signaling, we Moreover, RAMP2 modulates PTH1R downstream signaling in an agonist-dependent manner, most notably increasing the PTH-mediated Gi3 signaling sensitivity. These data uncover a critical role of RAMPs in the activation and signaling of a GPCR that may provide

protein-coupled receptors (GPCRs) are integral membrane proteins crucial for sensing extracellular signals These receptors initiate intracellular signaling cascades upon activation, ultimately regulating a myriad However, these conventional assays often provide limited information on intermediate signaling events due to pathway crosstalk and signal amplification [3]. Gilman, A.G., G proteins: transducers of receptor-generated signals. 

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greater understanding of how effector molecules interact with a receptor to initiate downstream effector signaling This review aims to explore the signaling pathways, dynamic structures, and physiological relevance in the cardiovascular system of the three most important GPCR signaling effectors: heterotrimeric G proteins is increasing appreciation for the elegance of the regulatory mechanisms that mediate intracellular signaling

October 2022 "The cAMP-dependent protein kinase (PKA) system represents a primary cell-signaling pathway PKA facilitates the actions of hormones, neurotransmitters and other signaling molecules that bind G-protein Through its control of synaptic events, exocytosis, transcriptional regulation, and more, PKA signaling Neural PKA signaling is regulated by afferent and peripheral efferent signals that link specific neural

A finely tuned signalling compartmentalization orchestrated in dynamic platforms is an essential requirement several studies have depicted the pivotal role of the cytoskeleton and lipid microdomains in controlling signalling Here, we discuss mechanisms responsible for signalling amplification and compartmentalization in T cell We also take into account the detrimental effect of mutations carried by distinct signalling proteins

Hi GPCR Community, If you work on GPCR discovery, you already know: early signals can mislead, and timing Industry insights:  Biopharma returns to MC4R; Recursion completes Exscientia acquisition, signaling Must-read publications:  β-arrestin2-biased allosteric modulator for pain beyond opioids & GPR3 regulated Why it matters now: Cleaner signal:  Selective excitation + low background reduces false positives in Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won

Through bioinformatic analysis of lysosomal proteomes, we identified lysosomal cholesterol signaling pathway for cholesterol sensing and couples cholesterol concentrations to mTORC1-dependent anabolic signaling

October 2022 High hedgehog signaling is transduced by a multikinase-dependent switch controlling the

October 2022 Structural perspectives on the mechanism of signal activation, ligand selectivity and allosteric

GPCRs show great diversity in their intracellular location, interacting partners and effectors, and signaling Here we will discuss recent studies on the diversity of location, effectors, and signaling of GPCRs, and how these could interact to generate specific spatiotemporal patterns of GPCR signaling in cells.

September 2022 GPCR/endocytosis/ERK signaling/S2R is involved in the regulation of the internalization However, its regulating signaling pathways remain to be elucidated. influence of specific inhibitors of G protein-coupled receptors (GPCR), endocytosis pathways, extracellular signal-regulated kinases 1/2 (ERK1/2) signaling, p38 signaling, mitochondrial respiration and Na+/K+-ATPase activity Overall, phagocytosis, CME, GPCR, ERK signaling, and S2R/TMEM97 are involved in the internalization of

encode a variety of bioactive small molecules with growing evidence for N-acyl amides as being important signaling Both groups of metabolites suppress anti-inflammatory interleukin-10 signaling in human macrophage cell

August 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer which interact directly and indirectly with a wide number of cellular partners and mediate downstream signaling adaptor proteins that control the recruitment, activation, and scaffolding of numerous cytoplasmic signaling complexes and assist in G-protein receptor signaling, thus bringing them into close proximity. This review delivers a concise overview of the role of β-arrestins with a primary emphasis on the signaling

October 2022 Genome-scale CRISPR screening reveals that C3aR signaling is critical for rapid capture

Sharpen your discovery decisions ➤ GPCR Signal Transduction Call for Papers: Define What Comes Next Volume As the GPCR field surges forward—from ligand bias to signaling diversity—the guest editors Dr. This is a chance to shape the next scientific consensus on how GPCRs work, signal, and fail. Our Premium Members don’t have to chase signals—they act on them. FAQ: What You Get with Dr. Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won

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discuss the historic context of pepducin development for each receptor, as well as the structural, signaling

Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein or β-arrestin signaling Although GPCRs are implicated in the pathophysiology of Alzheimer's disease (AD), biased GPCR signaling Our previous work demonstrated that GPR3-mediated β-arrestin signaling modulates amyloid-β (Aβ) generation reduced fertility, and memory impairment, which are potentially associated with impaired G protein signaling We further determined that G protein-biased signaling reduces soluble Aβ levels and leads to a decrease

October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR) signaling maintaining the spacing between ROS discs, suggesting a plausible mechanism by which intrinsic optical signals

with GPR108 and promoted its degradation, knockout of GPR108 remarkably blocked GA inhibition of NF-κB signaling

September 2022 Biased GPCR signaling by the native parathyroid hormone-related protein 1 to 141 relative variants of 139, 141, and 173 amino acids, our current understanding on how endogenous PTHrP transduces signals and (iii) receptor internalization and recycling that the native PTHrP1-141 displays biased agonist signaling Furthermore, we show that the molecular basis for biased signaling differences between PTHrP1-36 and Taken together, our results contribute to a better understanding of the biased signaling process of a

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GPR15 signals through the Gi/o pathway to decrease intracellular cyclic adenosine 3',5'-monophosphate -81) are used as pharmacological tool compounds to delineate the GPR15 receptor-mediated Gα protein signalling Furthermore, the GPR15 receptor signals through Gi/o to inhibit cAMP accumulation, which could be blocked