Adenylyl cyclase via activation. Medical search. Frequent questions

Previously, a model based on the structure of adenylate cyclase was used to predict the structure of the nucleotide-binding pocket of a membrane guanylyl cyclase, RetGC-1. (embl.de)
Despite widespread distribution in most mammalian cells, the role of soluble guanylate cyclase has, until recently, been poorly defined, especially when compared with its more illustrious sibling, adenylate cyclase. (embl.de)
Regulation of Adenylate Cyclase of Neuroblastoma x Glioma Hybrid Cells by a-Adrenergic Receptors. (nih.gov)

Leu5]-Enkephalin and selective delta- and mu-, but not kappa-, opioid receptor agonists inhibit the FSK stimulation of adenylyl cyclase activity with the same potencies displayed in stimulating basal enzyme activity. (unica.it)
Similarly, the muscarinic inhibition of FSK-stimulated adenylyl cyclase activity shows agonist and antagonist sensitivities similar to those characterizing the muscarinic stimulation of basal enzyme activity. (unica.it)
Fluoride stimulation of adenylyl cyclase is not affected by either carbachol or [Leu5]enkephalin. (unica.it)
Loss of one component in this complex leads to a defect in cAMP pathway activation in response to DA D 1 or adenosine A 2A receptor stimulation. (medscape.com)
Similar results were obtained after pharmacological stimulation of the adenylyl cyclase with forskolin. (jneurosci.org)
Thyroid cell growth and function are regulated by several hormones and growth factors that bind to cell surface receptors coupled via G proteins, Gs and Gq, to stimulation of adenylyl cyclase and phospholipase C (PLC), respectively. (nih.gov)
Activated Gs alpha causes constitutive stimulation of adenylyl cyclase and increases levels of intracellular cAMP. (nih.gov)
Because G protein-coupled signaling pathways exhibit cross-talk, we compared TG8 cells to FRTL-5 cells transfected with the neomycin resistance gene (TG4) to determine whether constitutive stimulation of adenylyl cyclase influences the PLC pathway. (nih.gov)
In addition, BRL 37344 and propranolol, ligands that act as agonists in the stimulation of cyclase, act as antagonists for ERK activation. (aspetjournals.org)
A beta -3 AR-mediated stimulation of PI3K is confirmed by the observation that the selective agonist CGP 12177A specifically activates protein kinase B. As was observed for the activation of ERK, the activation of protein kinase B is inhibited by preincubation with pertussis toxin and PI3K inhibitors, suggesting that both are a consequence of a G i/o -mediated activation of PI3K. (aspetjournals.org)
Bouaboula M., Poinot-Chazel C., Bourrié B., Canat X., Calandra B., Rinaldi-Carmona M., Le Fur G., Casellas P. (1995) Activation of mitogen-activated protein kinases by stimulation of the central cannabinoid receptor CB1. (adicciones.es)
however, the common thread is either stimulation or inhibition of adenylyl cyclase. (pharmacology2000.com)
These effects are mediated by the type A2A adenosine receptor via stimulation of adenylyl cyclase, increased production of cAMP, and activation of PKA. (nih.gov)

However, in the present study, we show that in the same brain area activation of these receptors causes inhibition of adenylyl cyclase activity stimulated by Ca2+ and calmodulin (CaM) and by forskolin (FSK), two direct activators of the catalytic unit of the enzyme. (unica.it)
Once released from presynaptic axonal terminals, DA interacts with at least five receptor subtypes in the central nervous system (CNS), which have been divided into two groups: the D1-like receptors (D1Rs), comprising D1 and D5 receptors, both positively coupled to adenylyl cyclase and cAMP production, and the D2-like receptors (D2Rs), comprising D2, D3, and D4 receptors, whose activation results in inhibition of adenylyl cyclase and suppression of cAMP production. (genome.jp)
Usually, activation of the five dopamine receptors (D 1 -D 5 ) proceeds via stimulations or inhibition of adenylyl cyclase (AC) mediated by Gs/olf or Gi/o signalling proteins respectively. (pharmacology2000.com)
Large number of extracellular signals is received by plasma membrane receptors which, upon activation, transduce information into the target cell interior via trimeric G-proteins (GPCRs) and induce activation or inhibition of adenylyl cyclase enzyme activity (AC).Receptors for opioid drugs such as morphine (micro-OR, delta-OR and kappa-OR) belong to rhodopsin family of GPCRs. (unimib.it)

Activation of opioid and muscarinic receptors stimulates basal adenylyl cyclase but inhibits Ca2+/calmodulin- and forskolin-stimulated enzyme activities in rat olfactory bulb. (unica.it)
G αi inhibits adenylyl cyclase to decrease cAMP production. (medscape.com)
ADP activates G-protein-coupled receptor (GPCR) signaling mediated by two metabotropic purinergic receptors in platelets, Gq-coupled P2Y 1 receptor activates phospholipase C whereas Gi-coupled P2Y 12 receptor inhibits adenylyl cyclase and activates PI-3K/Akt and ERK [ 5 ]. (hindawi.com)
Adenylyl cyclase enhances cyclic adenosine monophosphoate (cAMP) which activates protein kinase (PKA) that inhibits platelet shape change, granule secretion, calcium mobilization, and aggregation [ 6 ]. (hindawi.com)
Increased cyclic adenosine 3',5'-monophosphate inhibits G protein-coupled activation of phospholipase C in rat FRTL-5 thyroid cells. (nih.gov)
METHODS: Because we recently demonstrated that PKA activation inhibits the TNF-a sheddase, TNF-a-converting enzyme (TACE), we hypothesized that an alcohol-mediated PKA pathway blocks TACE activity and prevents the normative inflammatory response to hog barn dust exposure. (cdc.gov)

One recent study has reported that in medium spiny neurons, cAMP pathway activation is not dependent on the classical G s GTP-binding protein but requires a specific G protein subunit heterotrimer containing G αolf/β2/γ7 in particular association with adenylyl cyclase type 5. (medscape.com)
Finally, we are investigating some aspects of the signaling pathway that triggers autophagy and inflammasome activation in macrophages and other cell types. (nih.gov)
Our findings reveal an essential role of Ae2 in mouse spermiogenesis and stress the recently postulated involvement of bicarbonate in germ-cell differentiation through the bicarbonate-sensitive soluble-adenylyl-cyclase pathway. (cun.es)
To delineate these effects, we used PKA pathway inhibitors (adenylyl cyclase [AC], cAMP, and PKA) to modulate the effects of alcohol on dust-stimulated TNF-a release in the bronchial epithelial cell line, BEAS-2B. (cdc.gov)
CONCLUSIONS: These data suggest that alcohol requires a soluble cyclase-generated cAMP-PKA pathway that is dependent upon the action of NO to inhibit TACE and TNF-a release. (cdc.gov)
In this review Adrian Hobbs outlines some of the reasons why the soluble guanylate cyclase-cGMP pathway has remained outside the signalling spotlight for much of the past 30 years. (embl.de)
Here, by measuring activation of the MAPK pathway downstream of GPCR-Gαs-cAMP signaling, we show that the expression levels of PKI proteins can alter the balance of activation of two major cAMP targets: PKA and EPAC. (nih.gov)

[ 80 ] Furthermore, withdrawal from µ-opioids or cocaine following their chronic administration leads to an upregulation of adenylyl cyclase-mediated signaling, resulting in high levels of cAMP, which acts as a substrate for the endogenous production of adenosine. (medscape.com)
In animals treated with addictive drugs, cAMP, produced by DA D 1 receptor activation, was metabolized to extracellular adenosine. (medscape.com)
Owing to this, the adenosine tone was increased in slices from drug-treated animals and was entirely dependent on tonic activation of D 1 receptors. (medscape.com)
Beta2-receptor activation leads to activation of adenylyl cyclase and increased intracellular cyclic adenosine monophosphate (AMP). (medscape.com)
9. Interaction of early growth response protein 1 (Egr-1), specificity protein 1 (Sp1), and cyclic adenosine 3'5'-monophosphate response element binding protein (CREB) at a proximal response element is critical for gastrin-dependent activation of the chromogranin A promoter. (nih.gov)
12. Mitogen-activated protein kinase and protein kinase A signaling pathways stimulate cholecystokinin transcription via activation of cyclic adenosine 3',5'-monophosphate response element-binding protein. (nih.gov)
The binding of GTP then stimulates adenylyl cyclase, thus increasing intracellular cyclic 3 ,5 -adenosine monophosphate (cAMP). (jaycampbell.com)

Vilanterol is a long-acting beta agonist (LABA) that stimulates intracellular adenyl cyclase (catalyzes the conversion of ATP to cyclic AMP). (medscape.com)

Soluble adenylyl cyclase mediates hydrogen peroxide-induced changes in epithelial barrier function. (nih.gov)
The soluble adenylyl cyclase inhibitor, KH7, however, significantly increased the inflammatory response to hog barn dust. (cdc.gov)
Guanylate cyclase is found both in the soluble and particulate fractions of eukaryotic cells. (embl.de)
The soluble forms of guanylate cyclase are cytoplasmic heterodimers having alpha and beta subunits. (embl.de)
Soluble guanylate cyclase: the forgotten sibling. (embl.de)
He goes on to describe how new molecular biological and biochemical approaches have facilitated a characterization of soluble guanylate cyclase and how this enzyme has acquired a profound physiological significance, and much research attention, as the intracellular 'receptor' for nitric oxide. (embl.de)

Structure, mechanism, and regulation of mammalian adenylyl cyclase. (embl.de)

In rat olfactory bulb, muscarinic and opioid receptor agonists stimulate basal adenylyl cyclase activity in a GTP-dependent and pertussis toxin-sensitive manner. (unica.it)
These results indicate that in rat olfactory bulb delta- and mu-opioid receptors and muscarinic receptors, likely of the M4 subtype, can exert a dual effect on cyclic AMP formation by interacting with pertussis toxin-sensitive GTP-binding protein(s) and possibly by affecting different molecular forms of adenylyl cyclase. (unica.it)
Recent studies have noticed a remarkable increase in cAMP after opioid receptor blockade with antagonists or by morphine withdrawal, a phenomenon explained as cAMP overshoot, superactivation, supersensitization or heterologous sensitization of adenylyl cyclase. (medscape.com)
[ 84 ] On the other hand, activation of µ-opioid releases G αi and Gβγ. (medscape.com)

Likewise, ADP-stimulated Gi-coupled P2Y12 receptor that activates mitogen-activated protein kinases (MAPKs) (ERK, JNK, and p38) and PI-3k/Akt signaling to arrive at similar scenario of platelet activation and aggregation [ 7 ]. (hindawi.com)
cAMP is converted via adenylyl cyclase (AC) and activates protein kinase A to phosphorylate intracellular proteins that mediate specific responses. (spandidos-publications.com)

In conclusion, activation of β-adrenergic receptors in stratum lacunosum-moleculare GABAergic networks reduces electrical synaptic transmission via a cAMP/PKA signaling cascade, and affects the degree of synaptic divergence within the circuit. (jneurosci.org)

We further showed that activation of both calcium-mobilizing and adenylyl cyclase-coupled GPCRs leads to transition of single spiking to bursting type of electrical activity. (nih.gov)
Overall, these results suggest that activation G i/o -coupled GPCRs expressed in the dorsal striatum, such as the DOR, by G-protein biased agonists may be a potential strategy to decrease voluntary alcohol consumption and β-arrestin recruitment is to be avoided. (frontiersin.org)
We hypothesized that one conceivable strategy to inhibit this alcohol-induced neuronal excitability is by activation of metabotropic, inhibitory G i/o -protein signaling pathways via G-protein-coupled receptors (GPCRs) expressed on neurons in this region. (frontiersin.org)

Modulation of forskolin-mediated adenylyl cyclase activation by constitutively active GS-coupled receptors. (nih.gov)
Trifluoperazine and W7 inhibited depolarization-induced gene expression but did not affect expression induced by the adenylyl cyclase activator forskolin. (jneurosci.org)

Overexpression of PKI and its subsequent repression of PKA dysregulates these signaling pathways, resulting in increased intracellular cAMP, and enhanced activation of EPAC and MAPK. (nih.gov)

We previously demonstrated that in neutrophils mTORC2 is required for the chemoattractant-mediated activation of the adenylyl cyclase 9 (AC9), which converts ATP into cAMP, and regulates back contraction through MyoII phosphorylation. (nih.gov)
When catechol amines act on these receptors it undergoes phosphorylation and activation of adenylyl cyclase system which then releases cAMP as secondary messenger. (egpat.com)
In an acute myeloid leukemia (AML) model, several identified compounds reduced cAMP efflux, appropriately modulated pathways that are responsive to cAMP elevation (cAMP-responsive element-binding protein phosphorylation, and deactivation of Very Late Antigen-4 integrin), and induced mitochondrial depolarization and caspase activation. (unm.edu)

This heterotrimeric structure is coupled to Gq/11 and necessitates agonist binding to both receptors for G protein activation with subsequent intracellular Ca 2+ release. (pharmacology2000.com)
Agonist activation of 5-HT7 leads to conformational change of the Gα subunit and a slow dissociation of the Gγ subunit from both the receptor and Gα. (norheart.no)

In addition to Delta9-THC and its synthetic analogs, CB1 and CB2 receptors are bound by endogenous eicosanoid ligands (e.g. anandamide), and signal via Gi/o alpha subunits to regulate adenylyl cyclase activity (generally inhibitory), ion channel activation, intracellular Ca2+ levels, nitric oxide synthase activation, and immediate early gene expression. (enzolifesciences.com)

Ethanol is known to enhance the activity of adenylyl cyclase (AC) in a number of cells and tissues. (nih.gov)
Our goals are to understand how G-protein-coupled receptors (GPCR) transduce signals to downstream effectors in immune cells, to discern the mechanisms that control these responses, and to determine the physiologic consequences of G-protein activation for lymphocyte function. (nih.gov)
2. Peptidergic activation of transcription and secretion in chromaffin cells. (nih.gov)
7. Insulin-like growth factor I-mediated activation of the transcription factor cAMP response element-binding protein in PC12 cells. (nih.gov)
Activation of the gene by KCl-induced depolarization or the calcium ionophore A23187 was dependent upon and synergistic with cAMP in PC12 and C6-glioma cells, but neither depolarization nor treatment with A23187 affected cAMP levels. (jneurosci.org)
The expression of HK-2 was regulated by the activation of ADRB2 in 4T1 breast cancer cells primarily at the posttranscriptional level. (snmjournals.org)
Increasing of malignancy of breast cancer cells after cryopreservation: molecular detection and activation of angiogenesis after CAM-Xenotransplantation. (researchsquare.com)
Aside from ASM rest, other ramifications of 2-AR activation have already been reported, including upsurge in ciliary beat-frequency, adjustments in vascular 850879-09-3 manufacture permeability, reduction in ACh launch, and modulation of immune system cells function [21,23]. (biopaqc.com)

Ulsund's research finds that the same domains responsible for this preassociation are involved in low potency activation of adenylyl cyclase . (norheart.no)

By contrast, immediate activation of adenylyl cyclase (AC) enhances ACh discharge. (biopaqc.com)

At the level of the DNA, depolarization- induced activation is conferred on the proenkephalin gene by a previously characterized cAMP-inducible enhancer. (jneurosci.org)
The consequences of cAMP elevation are mimicked by depolarization induced either by K+ or by glutamate receptor activation, both which elevate cAMP amounts in the RGCs by activating a calcium-dependent type-1 adenylyl cyclase (Xia et al. (estme.org)
Activation of GHRH receptors results in the opening of a sodium channel in the somatotrope, leading to its depolarization. (jaycampbell.com)

The authors hypothesized that G protein-coupled receptor/inhibitory G protein (G i ) activation leads to caveolin trafficking to mitochondria. (silverchair.com)

In all characterised eukaryote guanylyl- and adenylyl cyclases, cyclic nucleotide synthesis is carried out by the conserved class III cyclase domain. (embl.de)
Additionally, D 2 receptor activation reduces presynaptic dopamine synthesis and the reduction in dopamine release may be accounted for by decrease in neuronal firing frequency. (pharmacology2000.com)
Beta blockers decrease the renin release by blocking β1 receptors therefore activation of renin-angiotensin system and synthesis of angiotensin-II are prevented. (egpat.com)

The pharmacological profile of the ERK activation by the beta -3 AR differs significantly from its activation of adenylyl cyclase. (aspetjournals.org)

Here, we explore the hypothesis that dorsal striatal G i/o -protein activation is sufficient to reduce voluntary alcohol intake. (frontiersin.org)
Blocking adenylyl cyclase activity was sufficient to reduce effects of the most potent compounds. (unm.edu)

Berrendero F., García L., Hernández M.L., Romero J., Cebeira M., deMiguel R., Ramos J.A., Fernandez-Ruiz J.J., (1998) Localization of mRNA expression and activation of signal transduction mechanisms for cannabinoid receptor in rat brain during fetal development. (adicciones.es)

All sites were co-administered with a high dose of isoproterenol (100 μm) for 3 min to maximally induce β-adrenergic sweating (β-adrenergic sweating is significantly blunted by subsequent activations). (nih.gov)

Using a voluntary, limited-access, two-bottle choice, drink-in-the-dark model of alcohol (10%) consumption, we validated the importance of G i/o signaling in this region by locally expressing neuron-specific, adeno-associated-virus encoded G i/o -coupled muscarinic M 4 designer receptors exclusively activated by designer drugs (DREADD) in the dorsal striatum and observed a decrease in alcohol intake upon DREADD activation. (frontiersin.org)

Therefore, subsequent effects on adenylyl cyclase activity, protein kinase C activity and ionic channel activity do not occur. (pharmacology2000.com)

The activation of ERK1/2 is sensitive to pertussis toxin, suggesting that the beta -3 AR, in addition to its interaction with G s , can couple to G i/o . (aspetjournals.org)

Activation of D 2 receptors decreases cAMP (G i ), increases K + , and decreases voltage-gated Ca 2 + currents. (pharmacology2000.com)

However, ADP-induced adenylyl cyclase attenuation vanishes cAMP production which culminate in platelet activation. (hindawi.com)

At the injured vascular site, the exposed subendothelial collagen and von Willebrand factor (vWF) initiate platelet activation marked by the secretion of prothrombotic factors like ADP, thrombin, serotonin, and thromboxane A2 (TXA2) [ 3 ]. (hindawi.com)

1. Secretin activation of chromogranin A gene transcription. (nih.gov)
3. Neurotrophin activation of catecholamine storage vesicle protein gene expression: signaling to chromogranin a biosynthesis. (nih.gov)
14. Glucocorticoid activation of chromogranin A gene expression. (nih.gov)

CTA1 catalyzes ADP ribosylation of Gs alpha, which results in persistent activation of Gs alpha. (nih.gov)
This results in inhibition of cAMP mediated cardiac activation. (egpat.com)

One potential AUD treatment approach is to increase inhibition of the dorsal striatum, a brain region with observed increasing activation upon alcohol tasting in heavy alcohol drinking human subjects ( 2 ). (frontiersin.org)

This work reveals that PKCbetaII is required for mTORC2-dependent AC9 activation and back retraction during neutrophil chemotaxis. (nih.gov)
Activation of PAC was dependent both on photon fluence rate and duration of irradiation, between which reciprocity held well in the range of 2-50 μmol m-2 s-1 (total fluence of 1200 μmol m-2). (soken.ac.jp)
Intermittent irradiation also caused activation of PAC in a photon fluence-dependent manner irrespective of cycle periods. (soken.ac.jp)
Further research showed that 5-HT4-dependent cAMP increase was compartmented close to the contractile apparatus of the cell , in near proximity of troponin I. Phosphodiesterase 4 appears downregulated in heart failure, increasing the contribution of phospodiesterase 3 on cAMP activation. (norheart.no)
Accordingly, cAMP efflux inhibition should result in: cAMP accumulation, activation of cAMP-dependent downstream signaling, viability loss, and apoptosis. (unm.edu)

Photoactivated adenylyl cyclase (PAC) was first purified from a photosensing organelle (the paraflagellar body) of the unicellular flagellate Euglena gracilis, and is regarded as the photoreceptor for the step-up photophobic response. (soken.ac.jp)

Anatomy20

Organisms19

Diseases3

Chemicals and Drugs171

Analytical, Diagnostic and Therapeutic Techniques and Equipment9

Phenomena and Processes30

Technology, Industry, Agriculture1

Information Science3

Adenylate Cyclase3

Stimulation13

Inhibition of adenylyl cyclase4

Inhibits6

Pathway7

Adenosine7

Stimulates1

Soluble6

Regulation1

Opioid4

Activates2

Adrenergic receptors1

GPCRs3

Forskolin2

Intracellular cAMP1

Phosphorylation3

Agonist2

Subunits1

Cells8

Potency1

Enhances1

Depolarization3

Inhibitory G protein1

Synthesis3

Pharmacological1

Sufficient to reduce2

19981

Significantly1

Decrease1

Activity1

Pertussis1

Increases1

CAMP production1

Secretion1

Gene3

Results2

Alcohol1

Dependent5

Response1