, referred to as "SynTAMs" for synaptic targeting molecules, that enable localized perturbations of cAMP We show that locally restricted suppression of postsynaptic cAMP levels or of cAMP-dependent protein-kinase Retrograde trans-synaptic rabies virus tracing revealed that postsynaptic cAMP signaling is required Given that postsynaptic latrophilin adhesion-GPCRs drive synapse formation and produce cAMP, we suggest that spatially restricted postsynaptic cAMP signals organize assembly of postsynaptic specializations

A role for BET proteins in regulating basal, dopamine-induced and cAMP/PKA-dependent transcription in The D1 receptor (D1R) is a Gαs/olf-coupled GPCR which activates a cAMP/PKA/DARPP-32 signalling cascade is unknown whether BET proteins, or Brd4 specifically, are involved in transcriptional activation by cAMP We further found that cAMP/PKA signalling promotes Brd4 recruitment to dopamine-induced genes in striatal

August 2022 Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based The second messenger cyclic adenosine monophosphate (cAMP) is a key mediator in many GPCR signaling pathways Monitoring intracellular cAMP levels can help identify orthosteric agonists and antagonists, as well The GloSensor™ cAMP assay enables real-time monitoring of signaling downstream of many GPCRs. GloSensor™ version is optimal for measuring cytosolic cAMP.

This is the case for the parathyroid hormone (PTH) type 1 receptor (PTHR), which engages on sustained cAMP

Although PTHrP1-36 induces transient cAMP production, acute intracellular Ca2+ (iCa2+) release and β-arrestin recruitment mediated by ligand-PTHR interactions at the plasma membrane, PTHrP1-141 triggers sustained cAMP

We find that PFC astrocytes express receptors for dopamine but are unresponsive through the Gs/Gi-cAMP

melatonin receptors are expressed on airway smooth muscle; whether they regulate intracellular cyclic AMP (cAMP) and calcium concentrations ([Ca2+]i), which modulate airway smooth muscle tone; and whether they or the nonselective MT1/MT2 agonist ramelteon (10 µM) significantly inhibited forskolin-stimulated cAMP the melatonin MT2 receptor is expressed in ASM, and modulates airway smooth muscle tone via reduced cAMP

It is primarily coupled to the Gs protein, which leads to the production of cyclic AMP (cAMP). G proteins, such as Gi/o and Gq/11, leading to different downstream effects, such as inhibition of cAMP In contrast, exendin-P5, another GLP-1R agonist, is biased towards cAMP accumulation but with reduced resulting in an open conformation of the TM6-ECL3-TM7 axis, which is associated with their bias towards cAMP Tirzepatide is a full agonist for cAMP production at the GLP-1R which minimal ability to recruit β-arrestins

number of G protein-coupled receptors (GPCRs) are now thought to use endocytosis to promote cellular cAMP signaling that drives downstream transcription of cAMP-dependent genes. glucagon receptor (GCGR), which mediates physiological regulation of hepatic glucose metabolism via cAMP transit via EEA1-marked endosomes shown previously to be sites of GPCR/Gs-stimulated production of cAMP We further show that endocytosis potentiates cytoplasmic cAMP elevation produced by GCGR activation and

orchestrate downstream signaling events, including the modulation of cyclic adenosine monophosphate (cAMP Traditionally, second messenger assays measuring cAMP accumulation, calcium mobilization, and ERK phosphorylation 9]), receptor trafficking ( e.g FYVE assay [10]),  β-arrestin dynamics ( e.g FLAsH biosensor [11]), cAMP Jiang, L.I., et al., Use of a cAMP BRET sensor to characterize a novel regulation of cAMP by the sphingosine

Experimental approach: COS-7 cells were transfected with the human GLP-2R and assessed for cAMP accumulation To examine selectivity, COS-7 cells expressing human GLP-1 or GIP receptors were assessed for cAMP accumulation

effects of these modifications on key signaling events such as receptor recruitment, trimer dissociation, cAMP : Phosphorylation Hotspots: P Loop (Ser44, Ser47, Thr48): Impairs ligand-stimulated Gβγ release and cAMP Ser151, Tyr154, Tyr155): Phosphorylation at Tyr154 and Tyr155 impaired ligand-stimulated Gβγ release, cAMP

October 2022 "The cAMP-dependent protein kinase (PKA) system represents a primary cell-signaling pathway neurotransmitters and other signaling molecules that bind G-protein coupled receptors (GPCR) to modulate cAMP

ERK1/2), signal transducer and activator of transcription 3 (STAT3), cyclic adenosine monophosphate (cAMP ), Ras homolog family member A (RhoA), exchange protein activated by cAMP (Epac), and transient receptor

AVPR2 is a kind of G protein coupled receptor (GPCR) and mainly couples with Gαs protein leading to cAMP Their functionality in terms of cAMP production via Gαs protein coupling was decreased compared to the

GPR15 signals through the Gi/o pathway to decrease intracellular cyclic adenosine 3',5'-monophosphate (cAMP Furthermore, the GPR15 receptor signals through Gi/o to inhibit cAMP accumulation, which could be blocked

sheet: β-strand folding of phosphorylation clusters guides GPCR binding to arrestin Dietary dibutyryl cAMP supplementation regulates the fat deposition in adipose tissues of finishing pigs via cAMP/PKA pathway noncommittal on oral obesity med until phase 1 data arrive Form and Function - Consequences of subcellular cAMP

SPASM) technique to show that Gq proteins could bolster Gs dependent-β2-adrenergic receptor-mediated cAMP However, IP1 signalling through the non-cognate Gq was not important for the increased β2AR-Gs-mediated cAMP

dimeric β2-AR, but not monomeric β2-AR, in a resting state, resulting in the production of a resting cAMP

dimeric β2-AR, but not monomeric β2-AR, in a resting state, resulting in the production of a resting cAMP

Many G-protein-coupled receptors (GPCRs) including EP4 are localized in cilia for modulating cAMP signaling

functional studies with mutations of β1-AR residues show effects on the cellular signaling from β1-AR to the cAMP

Octopamine activated PxOctβ3, resulting in increased levels of intracellular cAMP.

To confirm the activity of the virtual hits, an in vitro assay was conducted, measuring cAMP levels at

Stimulation of AVPR2 with a selective agonist desmopressin promoted CRPC cell proliferation through cAMP

GLP-1R was functional, as stimulation with a GLP-1R agonist triggered an increase in intracellular cAMP

gene-related peptide-induced relaxation of human coronary arteries: A key role for Gβγ subunit instead of cAMP gene-related peptide-induced relaxation of human coronary arteries: A key role for Gβγ subunit instead of cAMP

to constitutively activate the Gαs protein without a ligand, which elevates the basal intracellular cAMP